Diversification Ready Pharma-Developed Compounds

A select offering of Pharma-Developed bioactive small molecules, both approved therapeutics/drug candidates and tool compounds, is tailored for potential use in Late Stage Functionalization. Selected for their heterocyclic functionality, these bioactive small molecules can be quickly diversified with Baran Diversinates to include new, relevant functionality (including fluorine) or bioconjugation linkers in one step.

More information on the Baran Diversinate line of Late Stage Functionalization reagents can be found at aldrich.com/diversinates.

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C0614 (±) Clopidogrel hydrogensulfate ≥98% (HPLC), powder Inhibits ADP-induced platelet aggregation; anti-thrombotic drug.
C3025 (±)-Chlorpheniramine maleate salt ≥99% (perchloric acid titration) H1 Histamine receptor antagonist.
K2753 (±)-Ketamine hydrochloride solid Selective NMDA glutamate receptor antagonist; veterinary anesthetic.
L1764 (±)-Lorazepam Anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.
D2521 (+)-cis-Diltiazem hydrochloride ≥99% (HPLC) Blocks slow, or L-type Ca2+ channels; regulates Ca2+ release from intracellular stores in neutrophils; stimulates 1,4-dihydropyridine binding to Ca2+ channels; coronary vasodilator.
SML0004 (S)-(+)-Clopidogrel hydrogensulfate ≥98% (HPLC) (S)-(+)-Clopidogrel hydrogen sulfate is an antithrombotic antiplatelet agent. It specifically and irreversibly inhibits the Purinoceptor P2Y12 subtype which inhibits ADP-induced platelet aggregation. (S)-(+)-Clopidogrel hydrogen sulfate is the active isomer.
SML0197 4E1RCat ≥97% (HPLC) 4E1RCat ilnhibits the eIF4F translation initiation complex by binding to IF4E b and inhibiting the interaction between IF4E:eIF4G (IC50 = 3.2 μM). In in vitro translation experiments using MDA-MB-231 cells, 4E1RCat dose dependently inhibited cap-dependent translation, led to a decrease in polysome and 80S ribosomal subunits and reduced levels of the eIF4F-dependant proteins Mcl-1 and c-Myc.
A6351 A-315456 >98% (HPLC), solid Selective α1D-adrenoceptor antagonist.
A9736 A-438079 hydrochloride hydrate ≥98% (HPLC) A-438079 hydrochloride hydrate is a selective P2X7 purinoceptor antagonist in both human and rat with minimal activity at 75 different G-protein-coupled receptors, enzymes, transporters, and ion channels tested.
A6476 ABT-418 hydrochloride powder, ≥98% (HPLC) Neuronal nicotinic acetylcholine receptor agonist with cognition enhancing and anxiolytic activities.
A9227 ABT-491 hydrochloride ≥98% (HPLC) Highly potent, selective and orally active platelet-activating factor (PAF) receptor antagonist. Ki = 0.6 nM in human platelets.
A5111 ABT-724 trihydrochloride ≥98% (HPLC)  
SML0131 ABT-751 hydrochloride ≥98% (HPLC) ABT-751 is an orally bioavailable vascular disrupting agaent (VDA) with a broad spectrum of antitumor activity. It binds to the colchicine binding site on beta-tubulin and inhibits polymerization of microtubules.
A1612 AF-353 hydrochloride ≥98% (HPLC), powder AF-353 is a potent antagonist of P2X3 homotrimers and P2X2/3 heterotrimers with a pIC50 range of 7.3 - 8.5. The compound does not affect other P2X family members at 300-fold excess concentrations. AF-353 significantly reversed pain behavior in a rat model of bone cancer pain.
A3230 AR-A014418 ≥98% (HPLC), solid Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that has been implicated in pathological conditions such as diabetes and Alzheimer′s disease. GSK3 inhibitor, AR-A014418, inhibits GSK3 (IC50 = 104 nM), in an ATP-competitive manner (Ki = 38 nM). AR-A014418 does not significantly inhibit cdk2 or cdk5 (IC50 > 100 μM) or 26 other kinases, demonstrating high specificity for GSK3.
SML0178 ARL-17477 dihydrochloride hydrate ≥98% (HPLC) ARL-17477 is an nNOS specific inhibitor. The IC50 against rat nNOS is 35 nM and it has 100-fold selectivity over endothelial and inducible isoforms. ARL-17477 penetrates the brain, and reduces infarct size and reduces cerebral blood flow in several different rodent models of ischemic brain injury.
SML0089 Abacavir sulfate ≥98% (HPLC) Abacavir sulfate is a Nucleoside analog reverse transcriptase inhibitor (NRTI); guanosine analog used to treat HIV and AIDS.
A4669 Acycloguanosine ≥99% (HPLC), powder Antiviral agent. Phosphorylation by herpes simplex virus thymidine kinase (HSV-TK) leads to the formation of acycloguanosine triphosphate that competitively inhibits the viral DNA polymerase.
Antiviral agent. Phosphorylation by herpes simplex virus thymidine kinase (HSV-TK) leads to the formation of acycloguanosine triphosphate that competitively inhibits the viral DNA polymerase. Acycloguanosine can be used to induce apoptosis in cells transfected with HSV-TK. Inhibits replication of cytomegalovirus by a mechanism that is independent of its phosphorylation by viral or cellular thymidine kinase.
A6730 Akt1/2 kinase inhibitor ≥98% (HPLC) Isozyme selective Akt1/2 kinase inhibitor. In in vitro kinase assays, Akt1/2 kinase inhibitor shows IC50 = 58 nM, 210 nM, and 2.12 mM for Akt1, Akt2, and Akt3, respectively, The inhibition appears to be pleckstrin homology (PH) domain-dependent and the Akt1/2 kinase inhibitor has no inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 μM.
A0232 Alfuzosin hydrochloride ≥98% (HPLC), solid Alfuzosin hydrochloride is an alpha-adrenergic blocker used to treat benign prostatic hyperplasia (BPH). It works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate.
A1862 Alpidem ≥98% (HPLC), powder Alpidem is a potent antagonist of peripheral benzodiazepine receptor (PBR) that is located on the outer mitochondrial membrane and interacts with the mitochondrial permeability transition (MPT) pore. Alpidem is an anxiolytic drug from the imidazopyridine family. Alpidem acts selectively on the α3 receptor subtype and to a lesser extent at the α1 subtype (Kd of 0.33nM and 1.67nM respectively), of the benzodiazepine receptor.
A8800 Alprazolam Alprazolam binds the GABAA receptor at the benzodiazepine site, which is different than the ligand-binding site at which GABA binds. Alprazolam has been shown to be an anxiolytic (anti-anxiety agent) as well as having anticonvulsant, muscle relaxant and antidepressant activity.
A129 Amoxapine Tricyclic antidepressant; inhibits uptake of norepinephrine; inhibits 5-HT2 serotonergic receptors.
A2736 Anastrozole ≥98% (HPLC) Anastrozole, which contains a triazole functional group, reversibly binds to the cytochrome P-450 component of aromatase. Binding interferes with the catalytic properties of aromatase, which results in inhibition of estrogen synthesis.
A9611 Atipamezole ≥98% (HPLC) Atipamezole is a selective α2 adrenergic blocker. Atipamezole is more potent than yohimbine; it is very selective for α2 adrenergic vs α1 sites, but not selelctive for α2 subtypes.
PZ0193 Axitinib ≥98% (HPLC) Axitinib (AG-013736) is an orally available, potent (picomolar) and selective tyrosine kinase inhibitor that blocks VEGF receptors 1, 2 and 3. The drug blocks VEGF-mediated endothelial cell survival, tube formation, and downstream signaling through endothelial nitric oxide synthase, Akt and extracellular signal-regulated kinase.
B8810 BAY 41-2272 ≥97% (HPLC) BAY 41-2272 is an activator of soluble guanylate cyclase at a novel, NO-independent regulatory site. BAY 41-2272 is the first product that stimulates sGC through a non-NO mechanism. BAY 41-2272 inhibits platelet aggregation and induces vasorelaxation without nitrate tolerance.
B9685 BAY 61-3606 hydrochloride hydrate ≥98% (HPLC), powder Spleen tyrosine kinase (Syk) inhibitor; anti-inflammatory. Syk plays a major role in inflammation pathways via receptors for the Fc portion of immunoglobulins, as well as B cell signaling. It is orally active, potent (Ki 7.5 nM), and highly selective for Syk vs other kinases (Lyn, Fyn, Src, Itk, Btk; Ki′s).
B3561 BAY 73-6691 ≥98% (HPLC), powder BAY 73-6691 was characterized in vitro as the first potent and selective inhibitor of phosphodiesterase 9 (PDE9), which is currently under preclinical development for the treatment of Alzheimer′s disease. This compound selectively inhibits human (IC50 = 55 nM) and murine (IC50 = 100 nM) PDE9 activity in vitro and shows only moderate activity against other cyclic nucleotide-specific phosphodiesterases. BAY 73-6691 alone did not significantly increase basal cGMP levels. The PDE9 inhibitor significantly potentiated the cGMP signals generated by sGC activating compounds such as BAY 58-2667 or 5-cyclopropyl-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-4-ylamine (BAY 41-2272) and induced leftward shifts of the corresponding concentration-response curves. The newly generated PDE9 reporter cell line show that BAY 73-6691 is able to efficiently penetrate cells and to inhibit intracellular PDE9 activity.†
PZ0022 BLI-489 hydrate ≥98% (HPLC) BLI-489 is a penem β-lactamase inhibitor, which has shown activity against class A, C, and D β-lactamases. BLI-489 is being tested in combination therapy for drug-resistant bacteria.
B9935 BMS-345541 ≥98% (HPLC), powder BMS-345541 is an IKB kinase (IKK) allosteric site inhibitor.
SML0121 BTZO-1 ≥98% (HPLC) BTZO-1 is a suppressor of cardiomyocyte apoptosis presumably by activation of antioxidant response element (ARE)-mediated gene expression. BTZO-1 binds to the macrophage migration inhibitory factor (MIF) that is required to activate the glutathione S-transferase Ya subunit (GST Ya) gene ARE.
PZ0187 Begacestat ≥98% (HPLC) Begacestat (GSI-953) is a selective β-secretase inhibitor that selectively inhibits cleavage of APP over Notch.
B3563 Bifonazole ≥98% (HPLC) Bifonazole is an imidazole-based anti-fungal agent with broad spectrum activity against many fungi, molds, yeast and some Gram-positive bacteria. Bifonazole inhibits ergosterol biosynthetic protein 28 and Cytochrome P450 2B4.
B7188 Blonanserin ≥98% (HPLC) Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic.
PZ0192 Bosutinib ≥98% (HPLC) Bosutinib (SKI-606) is an orally active; dual Src/Abl tyrosine kinase inhibitor with potent antiproliferative activity. It does not appear to inhibit c-Kit and PDGRF, which are thought to be the cause of numerous side effects in anticancer treatment with some other tyrosine kinase inhibitors.
B6434 Bretazenil ≥96% (HPLC), solid Bretazenil is a benzodiazepine partial agonist.
B7148 Buspirone hydrochloride 5-HT1A serotonin receptor agonist; anxiolytic.
C1619 CGS-9343B ≥98% (HPLC), powder CGS-9343B is a selective calmodulin antagonist with minimal protein kinase C or antidopaminergic activity. CGS-9343B is a potent inhibitor of calmodulin-activated (Type I) phosphodiesterase activity with IC50 in the nanomolar range.
SML0187 CJ-13610 ≥98% (HPLC) CJ-13,610 is a potent inhbititor of 5-lipoxygenase (5-LO) activity (IC50 = 70 nM).
CJ-13610 inhibits the biosynthesis of leukotriene B4 and regulates the IL-6 mRNA expression in macrophages. It reduces fibrosis and necroinflammation of liver in carbon tetrachloride-treated mice.
C9498 CL-82198 ≥98% (HPLC), powder CL-82198 is a selective inhibitor of MMP-13 that displays no activity at MMP-1, MMP-9 or TACE. It is also a selective S1′ pocket binder, binding within the entire S1′ pocket of MMP-13, docking with the morpholine ring adjacent to the catalytic zinc atom without zinc chelation.
PZ0100 CP-154526 hydrochloride ≥98% (HPLC) CP-154526 is a selective, non-peptide antagonist of corticotropin releasing factor receptors (CRF1).
PZ0101 CP-226269 ≥98% (HPLC) CP-226269 is a D4 dopamine receptor agonist with EC50 of 32 nM.
PZ0189 CP-316819 ≥98% (HPLC) CP-316819 is a potent glycogen phosphorylase inhibitor. (IC50 = 40 nM against human liver GPα.) Under low glucose conditions, CP-316819 facilitates glycogen utilization in the brain, prevents neuronal cell death and maintains brain electrical currents.
PZ0108 CP-335963 ≥98% (HPLC) CP-335963 is an aurora 2 kinase inhibitor, PDGF inhibitor, and anti-proliferative.
PZ0103 CP-346086 dihydrate ≥97% (HPLC) CP-346086 is microsomal triglyceride transfer protein (MTP, MTTP) inhibitor.
PZ0129 CP-380736 ≥98% (HPLC) CP-380736 is an inhibitor of the epidermal growth factor receptor (EGFR). EGFR is a tyrosine kinase that activates MAPK, JNK, and Akt pathways, and is an important mediator of several types of cancer, including lung cancer and glioblastoma multiforme.
PZ0148 CP-802079 hydrochloride hydrate ≥98% (HPLC) CP-802079 is a potent and selective glycine transporter type 1 (GlyT1) antagonist. Antagonists of GlyT1 increase levels of glycine in the synaptic cleft and, like direct glycine site agonists, they can augment NMDAR currents and NMDAR-mediated functions. CP-802,079 significantly increases the amplitude of the NMDAR currents and LTP.
PZ0104 CP-91149 ≥98% (HPLC) CP-91149 is a selective glycogen phosphorylase inhibitor.
PZ0102 CP-93129 dihydrochloride hydrate ≥98% (HPLC) CP-93129 is a potent and selective 5-HT1B agonist.
C4024 Carbamazepine powder Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site. Sodium channel inhibitor.
PZ0008 Celecoxib ≥98% (HPLC) Celecoxib is a non-steroidal, anti-inflammatory drug (NSAID) and a cyclooxygenase-2 (COX-2) selective inhibitor. Celecoxib is at least 10-20 times more selective for COX-2 over COX-1.
C1240 Chlormethiazole hydrochloride ≥98% (HPLC), powder GABAA agonist; glycine receptor modulator.
C4522 Cimetidine H2 histamine receptor antagonist; I1 imidazoline receptor agonist; anti-ulcer agent. Blocks cancer metastasis by inhibiting the expression of E-selectin on the surface of endothelial cells, thus blocking tumor cell adhesion.
C6239 Cinalukast ~98% (HPLC) Specific CysLT1 leukotriene receptor antagonist.
C6019 Clotrimazole Clotrimazole is a specific inhibitor of Ca2+-activated K+ channels. It is an antifungal azole. Clotrimazole is a derivative of imidazole and has similar antimicrobial action and activity to ketoconazole. It inhibits cytochrome P450-dependent 14α-demethylase, which is critical to ergosterol biosynthesis. The accumulated 14α-methylated sterols change the membrane structure of sensitive fungi, altering cell membrane permeability.
PZ0191 Crizotinib ≥98% (HPLC) Crizotinib (PF-02341066) is an ATP-competitive inhibitor of the receptor tyrosine kinases (RTKs) c-Met (hepatocyte growth factor receptor) and anaplastic lymphoma kinase (ALK). Crizotinib is a highly specific inhibitor of c-Met and ALK among > 120 different RTKs surveyed. Crizotinib was approved for treatment of a subtype of nonsmall-cell lung cancer (NSCLC) with ALK fusion mutations.
D5321 D36 hydrate ≥98% (HPLC) D36 is an androgen receptor (AR) allosteric antagonist with inverse agonist properties. D36 inhibits both wild-type and agonist-induced AR activity and antagonized AR in a hormone-refractory model.
D1944 D4476 ≥98% (HPLC), solid D4476 is a potent, selective ATP-competitive inhibitor of CK1 (casein kinase 1).
D8696 DMH4 >99.0% (HPLC) DMH4 is a potent VEGF inhibitor and an angiogenesis inhbitor. It is a selective VEGF inhibitor with an IC50 of 161 nM for VEGFR inhibition compared to 8000 nM for AMPK. Unlike the structurally similar DMH1, which is a selective BMP inhibitor, DMH4 shows little affinitiy for BMP with an IC50 of 3500 nM for BMPR-I.
PZ0180 Delavirdine mesylate ≥98% (HPLC) Delavirdine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). It is used as part of highly active antiretroviral therapy (HAART) for the treatment of human immunodeficiency virus (HIV) type 1.
D3821 Devazepide ≥98% (HPLC), powder Devazepide is a CCK1 (CCK-A) receptor antagonist and a CCK8 antagonist.
D1446 Dexrazoxane ≥95% (HPLC) Dexrazoxane is a cardioprotective compound against anthracyclines. It functions by inhibiting topoisomerase II without inducing DNA strand breaks. Dexrazoxane is a + enantiomer of razoxane.
D0899 Diazepam Benzodiazepine anxiolytic; prototype ligand for the GABAA receptor benzodiazepine modulatory site.
D6196 Dimebon dihydrochloride hydrate ≥98% (HPLC) Mechanism of neuroprotection and cognition enhancement is not certain, but Dimebon blocks both cholinesterase and the NMDA receptor simultaneously and also appears to block the action of neurotoxic β-amyloid proteins and inhibit L-type calcium channels, and may exert a neuroprotective effect by blocking a novel target that involves mitochondrial pores.
D9571 Dolasetron mesylate hydrate ≥98% (HPLC), powder Dolasetron mesylate hydrate is a highly specific and selective serotonin 5-HT3 receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors.
D9815 Doxazosin mesylate ≥97% (HPLC), powder α1-adrenoceptor antagonist; relaxes smooth muscles of the prostate
SML0186 Dp44mT ≥98% (HPLC) Dp44mT is an iron chelator that works as a selective anticancer agent. As other iron chelators it can serve as a therapeutic adjunct to doxorubicin treatment. Additionally Dm44mT possess DNA-damaging activity. It appears that that activity is mediated by top2a inhibition.
PZ0183 ERB-041 ≥98% (HPLC) ERB-041 is a potent, selective estrogen ERβ receptor agonist (IC50 ERβ: 5.4 nM; > 200-fold selective over ERα). ERβ plays a minor role in mediating estrogen action in the uterus, the hypothalamus/pituitary, the skeleton, and other classic estrogen target tissues. However, a clear role for ERβ has been established in the ovary, cardiovascular system, and brain as well as in animal models of inflammation including arthritis, endometriosis, inflammatory bowel disease, and sepsis. There is increasing interest in finding ERβ agonists for potential use in a variety of clinical applications without triggering classic estrogenic side effects.
PZ0011 Eletriptan hydrobromide ≥98% (HPLC) Eletriptan hydrobromide is a serotonin 5-HT1B/1D receptor agonist; second generation anti-migraine drug.
E2535 Eprosartan mesylate ≥98% (HPLC) Angiotensin II type 1 (AT1) receptor antagonist; anti-hypertensive.
E6530 Etomidate >98% (HPLC), powder Etomidate is a general anesthetic; potentiates GABAA transmission. The possible neuroprotective effect of etomidate against streptozotocin-induced (STZ-induced) hyperglycaemia were investigated in the rat brain and spinal cord. Etomidate treatment demonstrated neuroprotective effect on the neuronal tissue against the diabetic oxidative damage
F3806 Fadrozole hydrochloride ≥98% (HPLC) Fadrozole is a nonsteroidal aromatase inhibitor. Fadrozole is a very potent and highly selective inhibitor of the aromatase enzyme system in vitro and estrogen biosynthesis in vivo. It inhibited the conversion of [4-14C]androstenedione to [4-14C]estrone by human placental microsomes in a competitive manner (Ki = 1.6 nM). At a substrate concentration 3-fold the Km, Fadrozole was 180 times more potent, as an inhibitor, than aminoglutethimide (Cat. No. A9657), exhibiting half-maximal inhibition at 1.7 nM as compared to 0.3 μM. In vivo, Fadrozole lowered ovarian estrogen synthesis by gonadotropin-primed, androstenedione treated, immature rats by 90% at a dose of 260 μg/kg (PO). In vivo, Fadrozole leads to sequelae of estrogen deprivation (e.g. regression of DMBA-induced mammary tumors) without causing adrenal hypertrophy in adult rats. It blocked aromatase by 50% in human breast cancer homogenates, live breast cancer cells, human placental microsomes, and porcine ovarian microsomes at concentrations of 0.008 to 0.02 μM.
F7932 Famciclovir ≥98% (HPLC) Famciclovir is an antiretroviral guanosine analog used to treat herpesvirus infections and hepatitis B. Famciclovir is rapidly converted to penciclovir. Viral thymidine kinase phosphorylates penciclovir to a monophosphate form that celular kinases convert in turn to penciclovir triphosphate. Penciclovir triphosphate competitively inhibits viral DNA polymerase and thus viral replication. Prolonged administration can lead to resistance; it is often manifested as selection of pre-existing resistant strains with mutations in the reverse transcriptase domain of the DNA polymerase gene.
F6889 Famotidine H2 histamine receptor antagonist; anti-ulcer agent
F4303 Fiduxosin hydrochloride >98% (HPLC), solid α1-Adrenoceptor antagonist.
F8929 Fluconazole ≥98% (HPLC), powder Fluconazole is an antifungal agent. It is highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethyllation. Fluconazole is a potent inhibitor of CYP2C9. Fluconazole interferes with fungal ergosterol synthesis and downregulates the metallothionein gene.
F6300 Flumazenil >99% (HPLC), solid Highly specific benzodiazepine receptor antagonist.
G5918 GR 113808 ≥98% (HPLC), solid GR 113808 is a 5-HT4 serotonin receptor antagonist.
G5794 GR 79236X ≥99% (HPLC), solid A1 adenosine receptor agonist
SML0083 GSK 1059615 sodium salt hydrate GSK 1059615 is a phosphatidylinositol-3-kinases (PI3K) inhibitor. GSK 1059615 inhibits proliferation of breast cancer BT474 cells via four different mechanisms that include retinoblastoma 1 (RB1)-mediated cell cycle arrest, elevated forkhead box protein O1 (FOXO) signaling, deduced MYC and transferrin receptor (TFRC) signaling and decreased cellular metabolism. Additionally, GSK 1059615 can suppress cell proliferation by decreasing mitogen-activated protein kinase (MAPK) signaling and imparts sensitivity to phosphoinositide 3-kinase (PI3K) inhibitor in cells resistant to the protein kinase B or AKT inhibitor. GSK 1059615 functions as a druggable target to reduce radiation-induced apoptosis in NCCIT cells. GSK 1059615 has entered clinical trial in patients with solid tumors or lymphoma and refractory malignancies.
GSK 1059615 is a potent inhibitor of PI3 Kinase. (IC50 = 2 nM)
G5797 GSK0660 ≥98% (HPLC) GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (160 nM). GSK0660 is nearly inactive on PPARα and PPARγ with IC50s greater than 10 μM.
G0798 GSK1016790A ≥98% (HPLC) GSK1016790A is a novel and potent TRPV4 channel agonist. The TRPV4 (transient receptor potential vanilloid 4) member of the TRP superfamily has been implicated in numerous physiological processes. GSK1016790A elicited Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. It is 300 fold more potent than 4a-PDD (Cat. No. P8014).
G0673 GSK4112 ≥98% (HPLC) GSK4112 is a rev-erbα, (orphan nuclear receptor NR1D1) agonist, the first agent able to reset the circadian clock in a phase-dependent manner. Rev-erbα impacts the precision of the circadian clock by repressing target gene activities with the help of a nuclear receptor co-repressor complex (NCoR) and HDAC3. GSK4112 competes with heme (rev-erb′s natural ligand) and enhances co-repressor complex recruitment and thus, repression of transcription. suggests that pharmacological modulation through Rev-erb may provide new routes to treat metabolic diseases, especially disorders of adipogenesis regulated by rev-erba.
G5668 GW1929 hydrate >98% (HPLC), solid GW1929 is a high affinity agonist of PPAR-γ.
G0668 GW2974 ≥98% (HPLC), solid Potent and selective dual inhibitor of EGFR (IC50 = 0.016 mM) and ErbB-2 receptor tyrosine kinase.
G1421 GW405833 hydrochloride ≥98% (HPLC), solid GW405833 is a selective cannabanoid CB2 receptor agonist; analgesic. GW405833 binds with high affinity at both human and rat CB2 receptors (Ki′s 3.9 and 3.6 nM); acts as a partial agonist (50% inhibition of forskolin-stimulated cAMP formation compared to full agonist CP55,940). GW405833 has potent analgesic activity in rat models of inflammatory, neuropathic and incisional pain; devoid of CNS effects common with CB1 agonists.
G3420 GW441756 hydrochloride ≥97% (HPLC), powder, red Highly selective and potent TrkA kinase inhibitor. Orally active. IC50 = 2 nM
G2171 GW843682X ≥98% (HPLC), solid GW843682X is a polo-like kinase-1 (PLK1) and polo-like kinase-3 (PLK3) inhibitor with nanomolar activity. It shows potent inhibition of proliferation of a wide variety of tumor cell lines.
G2536 Ganciclovir ≥99% (HPLC), powder Ganciclovir is a pro-drug nucleoside analog that is activated by phosphorylation. It is useful in the study of gene therapy in cancer research.
Upon expression of a viral suicide gene encoding thymidine kinase, the non-toxic pro-drug is converted to a phosphorylated active analog and is incorporated into the DNA of replicating eukaryotic cells, causing death of the malignant dividing cell. The cell cycle is irreversibly arrested at the G2-M checkpoint. Gap junction involvement in the ganciclovir bystander effect has been studied. Ganciclovir has been used to study loss of telomeres and to evaluate sensitivity of viruses to antiviral treatments.
PZ0172 Gisadenafil besylate salt ≥98% (HPLC) Gisadenafil (UK 369003) is a PDE5 inhibitor. It is 80 fold selective over PDE6, and greater than 3000 fold selective over PDEs 1-4 and 7.
G117 Glipizide solid ATP-dependent K+ channel blocker.
G3796 Granisetron hydrochloride ≥98% (HPLC), solid Granisetron hydrochloride is a serotonin 5-HT3 receptor antagonist and antiemetic.
I2909 Indoramin hydrochloride ≥98% (HPLC), solid α1-adrenoceptor antagonist.
J3770 JNJ7777120 ≥98% (HPLC) JNJ7777120 is a potent, selective non-imidazole H4 histamine receptor antagonist.
UC280 Ketoconazole Antifungal agent
L1415 L-162,313 ≥95%, solid Non-peptide AT1 receptor agonist.
L9787 L-655,708 ≥98% (HPLC), powder Novel ligand selective for the benzodiazepine site of GABAA receptors which contain the α5 subunit.
L9169 L-838,417 ≥98% (HPLC) L-838,417 is a novel pharmacology with no efficacy at a 1 subtype, but is partial agonist with equal efficacy at α2, K3 and α5 subtypes.
SML0010 LY-334370 hydrochloride hydrate ≥98% (HPLC), powder LY-334370 hydrochloride is a selective 5-HT1F receptor agonist.
LY-334370 modulates the transmission in the mouse trigeminal system and inhibits the neuronal responses within rat Sp5C by inhibiting c-Fos activation. It shows efficacy in aborting migraine attacks.
L1170 LY-487379 hydrochloride ≥98% (HPLC) LY-487379 is a positive allosteric modulator of the metabotropic glutamate receptor mGluR2. EC50 = 1.7 μM. LY-487379 shows no intrinsic agonist or antagonist activity at hmGluR2 and has no activity at human mGluR3. LY-487379 markedly potentiates glutamate-stimulated [35S]GTPγS binding in a concentration-dependent manner at hmGluR2, shifting the glutamate dose-response curve leftward by 3-fold and increasing the maximum levels of [35S]GTPγS stimulation. LY-487379 has anxiolytic effects in fear-potentiated startle. This activity profile is useful in all symptom domains of schizophrenia.
L2545 LY225910 ≥98% (HPLC) Cholecystokinin is expressed in the gastrointestinal tract and the central nervous system. Cholecystokinin receptor type 2 (CCK2) is a GPCR that is highly expressed in brain and spinal cord. CCK2 is implicated in many brain processes, including mood, anxiety, and pain, through its modulation of GABA neurotransmission.

LY225910 is a potent, selective CCK2 antagonist. LY225910 blocks agonism of CCK2 by CCK-8S, the peptide agonist. LY225910 has been measured in multiple systems, including GABA efflux from cortical cultures, depolarization of spinal cord neurons (via potassium conductance), modulation of excitatory postsynaptic potentials (EPSPs) in nucleus accumbens slices, and enhancement of morphine analgesia.
L6670 LY266097 ≥98% (HPLC), powder LY266097 is a selective 5HT-2B antagonist with a pKI of 9.7 for the human cloned 5-HT2B receptor and a 100-fold greater selectivity for 5-HT2B than the human 5-HT2C and 5-HT2A.
L1295 Lamivudine ≥98% (HPLC), powder Lamivudine is a potent nucleoside analog reverse transcriptase inhibitor (nRTI). It is an analogue of cytidine, and can inhibit both types (1 and 2) of HIV reverse transcriptase as well as the reverse transcriptase of hepatitis B. It needs to be phosphorylated to its triphosphate form before it is active. 3TC-triphosphate also inhibits cellular DNA polymerase.
L8533 Lansoprazole ≥98% (TLC), powder Gastric proton pump inhibitor.
SML0042 Lazabemide hydrate ≥97% (HPLC) Lazabemide is a selective and reversible monoamine oxidase B (MAO-B) inhibitor and Anti-Parkinson. Also it inhibits monoamine uptake at high concentrations (IC50 values are 86, 123 and > 500 μM for noradrenalin, serotonin and dopamine uptake respectively).
Lazabemide is effective in treatment of Alzheimer′s disease and in combination with nicotine replacement therapy aids in smoking cessation.
L6545 Letrozole ≥98% (HPLC) Letrozole is a third generation nonsteroidal aromatase inhibitor. It is a competitive inhibitor of the aromatase enzyme system and thus inhibits the conversion of androgens to estrogens. Letrozole inhibits the aromatase enzyme by competitively binding to the heme of the cytochrome P450 subunit of the enzyme, resulting in a reduction of estrogen biosynthesis in all tissues.
PZ0159 MCOPPB trihydrochloride hydrate >98% (HPLC) MCOPPB trihydrochloride is a potent non-peptide nociceptin/orphanin FQ peptide (NOP)-receptor full agonist [or opioid-receptor-like-1 (ORL1) receptor agonist]. MCOPPB is the most potent novel non-peptide NOP full agonist in vitro and an orally potent anxiolytic in the mice. It inhibited signaling through the NOP receptor in the mouse brain, suggesting that it penetrated into the brain after it was orally administered. It did not affect locomotor activity or memory, nor did it contribute to ethanol-induced hypnosis.
M7571 MK-571 sodium salt hydrate ≥95% (HPLC) MK 571 is a potent and selective leukotriene D4 (LTD4) antagonist and ABCC multidrug resistance protein 1(MRP1) inhibitor. The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, mediate their actions through two distinct G-protein coupled receptors. LTD4 is the preferred ligand for the CysLT1 receptor, whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor. MK 571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively. MK 571 effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors. It potentially inhibits MRP1 and has been shown to overcome acquired arsenic tolerance.
M3074 MMPIP ≥98% (HPLC) MMPIP is a potent, selective, allosteric antagonist of metabotropic glutamate receptor 7 (mGluR7). It also displays intrinsic activity and acts as an inverse agonist.
M4699 MTEP hydrochloride ≥98% (HPLC) MTEP is a potent and highly selective antagonist for mGluR5.
M3935 Meloxicam sodium salt hydrate ≥98% (HPLC) Meloxicam, a member of the oxicam family, is a non-steroidal anti-inflammatory drug (NSAID) that shows 300-fold selectivity for cyclooxygenase-2 (COX-2) vs cyclooxygenase-1 (COX-1). Meloxicam has been shown to abolish thymulin-induced increases of cytokines and NGF in the liver of rats. Meloxicam also suppresses tumor growth and may be capable of antagonizing cachexia in vitro.
M137 Methysergide maleate salt solid Nonselective 5-HT1, 5-HT2, and 5-HT7 serotonin receptor antagonist; antimigraine.
M2696 Metyrapone ≥98% (HPLC), solid Metyrapone is a glucocorticoid synthesis inhibitor; a standard in assessing adrenal gland function especially in response to stress, as well as pituitary gland function. In addition to acting as a glucocorticoid synthesis inhibitor, Metyrapone also inhibits cytochrome P450-mediated prostaglandin ω/ω-1 hydroxylase activity and impairs learning and memory. Data shows results in activation of the sleep EEG and a robust decrease in quantitative delta sleep.
M2419 Midazolam maleate salt Sedative/Hypnotic; ligand for the GABAA receptor benzodiazepine modulatory site; CYP3A4 substrate.
M4659 Milrinone ≥97% (TLC), powder Phosphodiesterase type III inhibitor; cAMP-specific, cGMP-inhibitable; potent cardiotonic, positive inotropic vasodilator.
M4145 Minoxidil ≥99% (TLC) Activates ATP-activated K+ channels; vasodilator; slow or stop hair loss and promote hair regrowth.
M0443 Mirtazapine ≥98% (HPLC) Mirtazapine is a noradrenergic and specific serotonergic antidepressant (NaSSA). Mirtazapine agonizes selective adrenergic and serotonergic receptors so that both NE release and 5-HT1A mediated serotonergic signaling are increased.
SML0101 Montelukast sodium hydrate ≥98% (HPLC) Montelukast sodium hydrate is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. It is a subtype specific CysLT1 receptor antagonist.
D6068 N-[4-[(6,7-Dimethoxy-4-quinazolinyl)amino]phenyl]benzamide hydrochloride ≥98% (HPLC), solid Aurora Kinase Inhibitor
N4382 Nalidixic acid sodium salt powder Nalidixic acid sodium salt is an inhibitor of bacterial DNA polymerase (DNA gyrase) and avian myeloblastoma virus reverse transcriptase. Inhibits nucleic acid and protein synthesis in Saccharomyces cerevisiae.
N1415 Naratriptan hydrochloride ≥98% (HPLC) Naratriptan hydrochloride is a serotonin 5-HT1B/1D receptor agonist.
N0290 Nitazoxanide ≥98% (HPLC) Nitazoxanide is an inhibitor of pyruvate-ferredoxin oxidoreductase (PFOR); Antimicrobial recently found to kill both non-replicating and replicating mycobacteria. FDA approved anti-parasitic drug (2002). Recent work (C & EN Sept. 14, 2009, p. 28) highlights that NTZ kills non-replicating and replicating TB bacteria and no apparent resistance is detected.
O1141 Olanzapine ≥98% (HPLC) Olanzapine is a 5-HT2 serotonin and D1/D2 dopamine receptor antagonist.
O3639 Ondansetron hydrochloride dihydrate ≥98% (HPLC), powder 5-HT3 serotonin receptor antagonist
Ondansetron, (3RS)-9-methyl-3-[(2-methyl-1H-imidazol-1-yl) methyl] 1,2,3,9-tetrahydro-4H-carbazol-4-one hydrochloride dehydrate acts as a selective 5-hydroxytryptamine type 3 (5-HT3) serotonin receptor antagonist. It is used as an antiemetic to control nausea and vomiting associated with chemotherapy and radiotherapy.
P9248 PD 169316 ≥98% (HPLC), solid Potent, cell-permeable and selective p38 MAP kinase inhibitor (IC50 = 89 nM).
PZ0109 PD-161570 ≥98% (HPLC) PD-161570 is an inhibitor of human FGF-1 receptor tyrosine kinase.
PZ0114 PD-166866 ≥98% (HPLC) PD-166866 is a selective inhibitor of the FGF-1 receptor tyrosine kinase (FGFR1) with IC50 = 55 nM, and no effect on c-Src, PDGFR-b, EGFR or insulin receptor tyrosine kinases or MEK, PKC, and CDK4.
PZ0142 PD-180970 ≥98% (HPLC) PD-180970 is a potent inhibitor of the p210 Bcr-Abl tyrosine kinase.
PZ0158 PF 3845 hydrate ≥98% (HPLC) PF 3845 is a potent, irreversible inhibitor of fatty acid amide hydrolase (FAAH), the principle enzyme involved in the degradation of the endocannabinoid anandamide. The endocannabinoid system is a target for therapeutic pain relief. PF-3845 is a covalent inhibitor that carbamylates FAAH′s serine nucleophile. It high selectivity over other enzymes including FAAH-2. In mouse studies, PF-3845 has been shown to raise brain anandamide levels for up to 24 hr; and in a rat model it produced significant reduction of inflammatory pain..
PZ0155 PF-03716556 ≥98% (HPLC) potent, selective and reversible acid pump antagonist (H, K-ATPase)
PZ0188 PF-3644022 hydrate ≥98% (HPLC) PF-3644022 is a potent inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MK2; Ki = 3 nM). PF-3644022 inhibits TNFa and IL-6 production in LPS-stimulated human whole blood (IC50 = 1.6 and 10.3 μM, respectively) and blocks TNFα production and paw swelling in a streptococcal cell wall-induced arthritis in rats.
PZ0143 PF-4708671 ≥98% (HPLC) PF-4708671 is a selective p70 ribosomal S6 kinase (S6K1) inhibitor. PF-4708671 inhibits S6K1 with a Ki of 20 nM and IC50 of 160 nM, while having no effect on the closely related RSK and MSK kinases.
PZ0186 PF-477736 ≥98% (HPLC) PF-00477736 is a potent, selective ATP-competitive small-molecule inhibitor that inhibits Chk1 with a Ki of 0.49 nM. The compound abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin.
PZ0151 PF-956980 hydrate ≥98% (HPLC) PF-956980 is a FGF1 receptor antagonist; PDGF receptor modulator; Flt3 tyrosine kinase modulator; and VEGF antagonist.
PZ0178 PHA 767491 hydrochloride ≥98% (HPLC) PHA-767491 is a potent and selective ATP-competitive dual inhibitor cdc7/cdk9. PHA-767491 blocks DNA synthesis and affects the phosphorylation of the replicative DNA helicase at Cdc7-dependent phosphorylation sites.
PZ0135 PHA-543613 ≥98% (HPLC) PHA-543613 is a potent selective α7 nAChR agonist. Nicotinic acetylcholine receptors are ligand-gated ion channels activated by nicotine, expressed in multiple tissues, with high functional expression in brain. The homomeric subtype α7 is a potential therapeutic target for cognitive deficits in schizophrenia and Alzheimer′s disease. PHA-543613 is active in both in vitro (binding, calcium flux, patch-clamp) and in vivo (auditory gating, novel object recognition) assays.
P0043 PNU-120596 ≥98% (HPLC) An allosteric modulator of α7 nicotinic receptors, N-(5-chloro-2,4-dimethoxyphenyl)-N′-(5-methyl-3-isoxazolyl)-urea (PNU-120596), causes conformational changes in the extracellular ligand binding domain similar to those caused by acetylcholinePNU-120596 is a positive allosteric modulator selective for the α7 nicotinic acetylcholine receptor. PNU-120596 produces no detectable change in currents mediated by α4β2, α3β4, α9α10 nAChRs. It increases channel mean open time, but does not affect ion selectivity. It does not bind at the agonist binding site, but induces conformational changes similar to the natural effector.
SML0107 Pemirolast potassium ≥98% (HPLC) Pemirolast potassium is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent. It Inhibits chemical mediator release from tissue mast cells and has recently also been shown to inhibit the release of peptides including substance P, neurokinin (NK) A, and calcitonin gene-related peptide (CGRP) from sensory nerves. It has been used for the treatment of allergic conjunctivitis prophylaxis of for pulmonary hypersensitivity reactions to drugs such as paclitaxel
P8828 Pergolide mesylate salt ≥98%, solid Dopaminergic agonist; suppresses pituitary secretion of prolactin; anti-Parkinsonian agent.
P6503 Pilocarpine hydrochloride ≥98% (titration), powder Nonselective muscarinic acetylcholine receptor agonist; used to produce an experimental model of epilepsy.
P6628 Pilocarpine nitrate salt ≥98% (TLC), powder Nonselective muscarinic acetylcholine receptor agonist; used to produce an experimental model of epilepsy.
P0778 Pindolol ≥98% (TLC), powder β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator.
E6910 Pioglitazone hydrochloride ≥98% (HPLC) Pioglitazone hydrochloride is a PPARγ agonist and thiazolidinedione (TZD) anti-diabetic. Pioglitazone is a selective agonist of the nuclear receptor peroxisome proliferator-activated receptor γ (PPAR-γ) and to a lesser extent PPAR-α.
P9233 Piribedil maleate salt A direct dopamine agonist; may be selective for the D3 subtype; no significant affinity for D1 receptors.
B9688 Pizotifen ≥98% (HPLC) Pizotifen is a serotonin antagonist acting mainly at the 5-HT1, 5-HT2A and 5HT2C receptors with some antihistamine activity. It is used for the prevention of vascular headache including migraine and cluster headache.
P5514 Pyrilamine maleate salt H1 histamine receptor antagonist.
P0027 Pyrvinium pamoate salt hydrate ≥98% (HPLC) Pyrvinium pamoate is a potent androgen receptor inhibitor. Androgen receptors (ARs) are nuclear hormone receptors/transcription factors that reside in the cytoplasm and activated by testosterone and dihydrotestosterone. AR inhibitors have potential therapeutic benefit in prostate cancer; competitive inhibitors and chemical castration methods have been discovered, but both therapies have undesirable side effects and/or resistance potential. A screen for non-competitive inhibitors was performed, resulting in the discovery of pyrvinium as an AR inhibitor. In comparison to competitive inhibitors, this compound does not bind to the ligand-binding domain of AR or block DNA occupancy by AR, but it inhibits AR-dependent gene expression via a distinct signaling mechanism. It is more potent than classical competitive AR antagonists and exhibits synergy with other AR inhibitors.
Q0875 Quinidine sulfate salt dihydrate Class IA antiarrhythmic; potassium channel blocker.
Q3625 Quinidine anhydrous Class IA antiarrhythmic; potassium channel blocker.
Q1250 Quinine hemisulfate salt monohydrate synthetic, ≥90% (HPLC) Potassium channel blocker. Antimalarial, anticholinergic, antihypertensive, and hypoglycemic agent; alkaloid originally isolated from the Cinchona family of South American trees. Inhibits mitochondrial ATP-regulated potassium channel. Used to study the metabolism of biocrystalized heme, hemozoin, in malarial parasites and to study the toxicity of heme (FP)-complexes.
R2533 RS-127445 hydrochloride ≥98% (HPLC), powder RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi=9.5) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
R9156 Raltitrexed monohydrate ≥98% (HPLC), solid Raltitrexed is a folate-based inhibitor of thymidylate synthase (TS) that is rapidly and extensively metabolized to its more potent polyglutamate derivatives. By inhibiting the formation of precursor pyrimidine nucleotides, raltitrexed prevents the formation of DNA and RNA, which are required for the growth and survival of both normal cells and cancer cells.
R109 Ro 15-4513 solid Benzodiazepine receptor partial inverse agonist; anxiogenic; ethanol antagonist.
R8782 Ro4368554 ≥98% (HPLC) Ro4368554 is a 5-HT6 receptor antagonist. RO4368554 acts selectively at 5-HT6 receptors where it binds with a greater than 100-fold selectivity over other monoamine receptor subtypes (-log M pKi = 9.4 at 5-HT6 and 7.1 at 5-HT2A).
R2408 Rosiglitazone ≥98% (HPLC) Rosiglitazone is a potent agonist for PPARγ with an EC50 of 43 nM for the human receptor. It is antidiabetic, working as an insulin sensitizer by binding to the PPARγ receptors in fat cells and making the cells more responsive to insulin.
R9281 Rotigotine hydrochloride ≥98% (HPLC) Rotigotine is a dopamine receptor agonist with preference for D3 receptors over D2 and D1. As such, it is an effective anti-Parkinsonian agent. Racemic rotigotine is about 50 times as potent as quinpirole, the gold standard D2 agonist.
R8404 Rufinamide ≥98% (HPLC), powder Broad-spectrum anticonvulsant.
P152 S(–)-Pindolol solid β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator. Active enantiomer of pindolol.
C4915 S-(+)-Chlorpheniramine maleate salt H1 histamine receptor antagonist; active isomer.
Chlorpheniramine maleate is clinically used as a topical ointment to treat skin disorders such as sunburn, urticaria, angioedema, pruritus and insect bites.
P5749 S-(+)-PD 123177 trifluoroacetate salt hydrate ≥98% (HPLC), solid S-(+)-PD 123177 is selective AT2 angiotensin receptor antagonist. The angiotensin AT2 receptor is an atypical seven transmembrane domain receptor that is coupled to activation of tyrosine phosphatase and inhibition of MAP kinase, and does not undergo agonist-induced internalization. An investigation of the occurrence and nature of AT2 receptor phosphorylation revealed that phorbol ester-induced activation of protein kinase C (PKC) in HA-AT2 receptor-expressing COS-7 cells caused rapid and specific phosphorylation of a single residue (Ser354) located in the cytoplasmic tail of the receptor. Agonist activation of AT2 receptors by angiotensin II (Ang II) also caused rapid PKC-dependent phosphorylation of Ser354 that was prevented by the AT2 antagonist, S-(+)-PD 123177, and by inhibitors of PKC. In cells coexpressing AT1 and AT2 receptors, Ang II-induced phosphorylation of the AT2 receptor was reduced by S-(+)-PD 123177 and abolished by treatment with both antagonists or with PKC inhibitors. These findings indicate that the AT2 receptor is rapidly phosphorylated via PKC during homologous activation by Ang II, and also undergoes heterologous PKC-dependent phosphorylation during activation of the AT1 receptor.
S7076 SB 202190 monohydrochloride hydrate ≥98% (HPLC) SB 202190 binds within the ATP pocket of p38 kinase and inhibits the p38α and β isoforms.
SB 202190 is a highly selective, potent, and cell-permeable inhibitor of p38 MAP kinase.
S7067 SB 202190 ≥98% (HPLC) SB 202190 is a highly selective, potent and cell permeable inhibitor of p38 MAP kinase. SB 202190 binds within the ATP pocket of the active kinase (Kd = 38 nM, as measured in recombinant human p38), and selectively inhibits the p38α and β isoforms.
S0693 SB 204741 >98% (HPLC) 5-HT2B serotonin receptor antagonist.
S3442 SB 216763 >98% (HPLC) Potent, selective, cell permeable glycogen synthase kinase-3 (GSK-3) inhibitor.
SB-216763 is a small molecule that competes with ATP and potently inhibits the activity α and β isozymes of GSK-3. It acts as neuroprotectant and prevents neuronal cell death induced by PI3-kinase pathway. It also delays preconditioning, reduces infarct size and prevents cardiac ischemia.
S9070 SB 220025 trihydrochloride ≥98% (HPLC), solid SB 220025 is a potent, specific inhibitor of human p38 mitogen-activated protein (MAP) kinase, with an IC50 value of 60 nM and 50- to 1000-fold selectivity. SB 220025 reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 reduced the lipopolysaccharide-induced production of TNF at an ED50 value of 7.5 mg/kg. At 30 mg/kg, SB 220025 reduced the expression of TNF and inhibited angiogenesis by ~40%. In a further study, the effects of p38/CSBP MAP kinase inhibition in angiogenesis-dependent chronic inflammatory disease was tested in murine collagen-induced arthritis and SB 220025 was able to prevent the progression of established arthritis.
S0569 SB 239063 >98% (HPLC) Potent p38 MAP kinase inhibitor. Selective for α and β. No activity against γ and δ isoforms.
S8061 SB 242084 dihydrochloride hydrate ≥98% (HPLC), powder SB 242084 is a potent and selective antagonist of 5-HT2C receptor. It increases the basal activity of dopaminergic neurons and affects the behavioral responses mediated by 5-HT2C such as mesolimbic neuron activity and food intake.3,4,5
S4317 SB 431542 hydrate ≥98% (HPLC), powder Potent and selective inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors.
SB-431542 inhibits the TGF-β-mediated activation of SMAD proteins, expression of collagen and fibronectin, cell proliferation and cell motility. It does not inhibit kinases that are activated in response to serum or stress such as ERK, p38 or JNK.
S1068 SB-215505 solid, >98% (HPLC) Selective 5-HT2B serotonin receptor antagonist; 100-fold higher affinity at 2B versus 2C.
S2694 SB-408124 ≥98% (HPLC), solid SB 408124 is an OX1 orexin receptor antagonist.
SB-408124 blocks the orexin type 1 receptor that stimulates the production of stress hormone in hypothalamus. It blocks orexin A-induced increase in arterial pressure and elevation of heart rate in rats. SB-408124 modulates phrenic nerve activity that is important in respiration.
S4696 SB-505124 hydrochloride hydrate ≥98% (HPLC) SB-505124 is an inhibitor of activin receptor-like kinase (ALK) 5, also known as transforming growth factor-α type I receptor kinase, with an IC50 of 47 ± 5 nM.
SB-505124 selectively inhibits TGF-β type I receptors, activin receptor-like kinases (ALK) 4, 5 and 7. It inhibits ALK4-, 5- and 7-mediated activation of Smad2, Smad3 and MAPK pathway induced by TGF-β.1 SB-505124 inhibits the human fibroblast trans-differentiation induced by the co-culture with Esophageal squamous cell carcinoma.2
S8822 SB-525334 ≥98% (HPLC) SB-525334 blocks the activation of Smad2/3 induced by TGFβ1 in renal proximal tubule cells.4 The sensitivity of TGFβ1 is decreased by SB-525334 that benefits the pulmonary arterial hypertension condition by reversing the pulmonary arterial pressure.5 SB-525334 is reduces the tumor incidence and size of mesenchymal tumors such as uterine leiomyoma.6
SB-525334 is a potent activin receptor-like kinase (ALK5)/ type I TGFβ-receptor kinase inhibitor with IC50 = 14.3 nM.
PZ0106 SC-236 ≥98% (HPLC) SC-236 is a cyclooxygenase-2 (COX-2) inhibitor.
PZ0176 SC-26196 ≥98% (HPLC) SC-26196 is a Delta6 fatty acid desaturase (Delta6D) inhibitor. It specifically inhibited Delta6D activity with an IC(50) value of 100 nM. The rate-limiting step in arachidonic acid synthesis is the desaturation of dietary linoleic acid by Delta6D. SC-26196 completely prevented this conversion of linoleic acid to arachidonic acid.
PZ0138 SC-51089 hydrate ≥98% (HPLC) SC-51089 is a selective EP1 prostanoid receptor antagonist.
SML0179 SR 27897 hydrate ≥98% (HPLC) SR 27897 has good brain accessibility and regulates the ileal motility through effects on peripheral nervous system.
SR 27897 is a potent, selective antagonist of the Cholecystokinin (CCK) receptor CCK1. SR-27897 blocks the elevation of leptin levels in the CNS following injection of CCK-8 peptide, and causes an increase in food intake in rats.
S8072 Sertindole ≥97.5% (HPLC) Sertindole is a 5-HT2 serotonin and D2 dopamine receptor antagonist and antipsychotic.
Sertindole readily passes the blood-brain barrier and is metabolized into compounds that show greater affinity for 5-HT2 receptors and less for D2 receptors. It is an effective treatment agent for schizophrenia as it improves cognitive impairment.1 Sertindole also acts as antagonist to human cardiac potassium channel, HERG and produces prolonged QT interval.2
S1198 Sumatriptan succinate ≥98% (HPLC), solid Sumatriptan succinate is a 5-HT1 serotonin receptor agonist.
T3955 TNP ≥95% (HPLC) TNP is a potent and selective IP6K inhibitor; less selective inhibitor of IP3K. Discovery of TNP as an inositol trisphosphate (IP3) kinase inhibitor was first reported in 2002, However, a recent reference shows that TNP is more potent as an IP6K inhibitor, making it valuable for study of inositol pyrophosphates.
T1452 TPCA-1 ≥95% (HPLC) TPCA-1 is a potent and selective inhibitor of human IκB kinase-2 (IKK-2) with IC50 = 17.9 nM for IKK-2 compared to 400nm for IKK-1. It has been used to study inhibition of IKK-2 to prevent inflammatory mediator release in animal models of arthritis and airway inflammation.
T6704 Tandospirone ≥98% (HPLC) Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner. The potency of tandospirone is equal to that of buspirone and approximate half that of diazepam. The potency of tandospirone as a dopamine antagonistic is less than 1/4 that of buspirone.
T2577 Temozolomide ≥98% (HPLC) Temozolomide is a DNA methylating agent and drug resistance-modifying agent; anti-tumor and anti-angiogenic. Temozolomide induces G2/M arrest and apoptosis through adduction of a methyl group to O6 position of guanine in genomic DNA and functional inactivation of DNA repair protein O(6)-alkylguanine DNA alkyltransferase (AGT) in base excision repair (BER) pathway.
T1633 Theophylline anhydrous, ≥99%, powder Phosphodiesterase inhibitor; diuretic; cardiac stimulant; muscle relaxant; asthma medication.
Theophylline is a tea alkaloid that functions as a nonselective PDE4 inhibitor. It can induce smooth muscle relaxation in the bronchiolae of asthma patients. At increased concentrations, theophylline can function as a reprotoxic agent and can cause infertility by incapacitating Sertoli cells. This subsequently causes the premature release of late differentiating spermatogenic cells.
SML0035 Tiagabine hydrochloride ≥98% (HPLC) Tiagabine hydrochloride is an anticonvulsant and selective GABA reuptake inhibitor through inhibition of the synaptic GABA transporter GAT1.
Tiagabine increases the synaptic GABA and enhances the neuronal inhibition. It is effective as adjunctive treatment of epilepsy and anxiety disorders.
T3202 Torsemide ≥98% (HPLC), solid Torsemide functions in the thick ascending limb of the loop of Henle and enhances the excretion of sodium, chloride and water from the luminal side of the cells. Furthermore, torsemide can treat oedematous conditions that are associated with diseases such as liver cirrhosis, kidney disorders and chronic congestive heart failure2.
Torsemide is a loop diuretic of the pyridine-sulfonylurea class with antialdosteronergic properties and inhibitor of the Na+/K+/2Cl- carrier system.
T6764 Triprolidine hydrochloride ≥99% H1 histamine receptor antagonist.
T104 Tropisetron monohydrochloride solid, ≥98% (HPLC) 3-Tropanylindole-3-carboxylate hydrochloride is a selective 5-HT3 serotonin receptor antagonist.
Tropisetron a selective serotonin 5-HT3 receptor antagonist is used mainly as an antiemetic to treat nausea and vomiting following chemotherapy . In the treatment of fibromyalgia syndrome (FMS) tropisetron reduced not only pain perception but also had a favourable effect on cardiac dysfunction during treatment.
SML0191 Valganciclovir hydrochloride hydrate ≥98% (HPLC) Valganciclovir hydrochloride hydrate is an antiviral used to treat cytomegalovirus infection. It is the prodrug of ganciclovir, a synthetic analog of 2′-deoxy-guanosine which is phosphorylated to a dGTP analog that competitively inhibits the incorporation of dGTP by viral DNA polymerase.
Valganciclovir is a valine ester of Ganciclovir, used to treat cytomegalovirus retinitis in HIV-infected patients. It is rapidly metabolized to ganciclovir by hydrolysis before entering the systemic circulation resulting in improved absorption of the drug.
PZ0004 Varenicline tartrate ≥98% (HPLC) Varenicline tartrate is a partial α4β2 nicotinic receptor agonist and α7 full agonist. Varenicline competitively binds to α4β2 receptors and partially stimulates without creating a full nicotine effect, while simultaneoudly blocking the ability of nicotine to bind to the receptors. Varenicline thus blocks the ability of nicotine to activate α4β2 receptors and stimulate the central nervous mesolimbic dopamine system, believed to be the neuronal mechanism underlying reinforcement and reward experienced upon smoking.
PZ0005 Voriconazole ≥98% (HPLC) Voriconazole is an antifungal used to treat serious fungal infections. Voriconazole inhibits ergosterol synthesis by inhibiting CYP450-dependent 14-α sterol demethylase resulting in a depletion of ergosterol in fungal cell membranes.
X2254 XE-991 ≥98% (HPLC) XE-991 is a KCNQ channel blocker; which is more potent than linopiridine (Cat. No. L-134).
X3129 XRP44X ≥98% (HPLC) XRP44X is a Ras-Net (Elk-3) pathway inhibitor; tubulin polymerization inhibitor Colchicine binding site.
Z4152 Zafirlukast ≥98% (HPLC) Zafirlukast is a potent subtype specific cysteinyl leukotriene type 1 receptor (CysLT1) antagonist; antiasthmatic. Zafirlukast has over 1000-fold selectivity for CysLT1, one of two receptors for cysteinyl leukotrienes LTC4, LTD4, and LTE4, which are important mediators of human bronchial asthma.
Z0502 Zaleplon ≥98% (HPLC), solid Zaleplon is a non-benzodiazepine agonist at the benzodiazepine site of the GABAA receptor; sedative; hypnotic.
Z101 Zimelidine dihydrochloride solid Serotonin transport blocker; antidepressant.
Z103 Zolpidem ≥98% (HPLC), solid Potent and selective agonist for the benzodiazepine receptor associated with the GABAA receptor; hypnotic.
SML0076 Zoniporide hydrochloride hydrate ≥98% (HPLC) Zoniporide is a potent and selective inhibitor of Na+/H+ exchanger isoform 1 (NHE-1). IC50 = 59 nM at NHE-1, vs. 12,000 nM at NHE-2; Zoniporide inhibits NHE-1-dependent Na+ update with IC50 of 14 nM.
Zoniporide, a selective inhibitor of sodium-hydrogen exchanger isoform 1 (NHE-1) has cardioprotective effects against myocardial injuries and ischemic insults. It inhibits the swelling human platelets and attenuates cardiac contractile dysfunction in rats. Zoniporide might have neurotoxic effects as it causes peripheral sensory axonopathy.
A2734 α5IA ≥98% (HPLC) α5IA is a selective inverse agonist for Α5 subtype of GABAA receptor with a higher intrinsic activity at the A5 subtype than other drugs. α5IA enhances cognition in laboratory animals without being proconvulsant or anxiogenic. α5IA acts as an "alcohol antagonist," markedly reducing the amnesic effect of alcohol and partially attenuating sedation, similar to Ro15-4513, but without the anxiogenic effect. α5IA offers promise as a tool to study cognitive disorders, memory function, and treatment of alcohol-related disorders.