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A6719   ω-Agatoxin IVA ≥90% (HPLC) Mutations in the CACNA1A (calcium voltage-gated channel subunit alpha1 A) gene is responsible for episodic ataxia 2, familial hemiplegic migraine type 1 (FHM1) and spinocerebellar ataxia type 6 (SCA6).
Toxin found in the venom of the funnel web spider, Agelenopsis aptera. Potent, selective blocker of mammalian P-type voltage-dependent calcium channels.
human ... CACNA1A(773)
mouse ... CACNA1A(12286)
rat ... CACNA1A(25398)
A5605 Amlodipine besylate ≥98% (HPLC) Amlodipine is an L-type calcium channel blocker. Amlodipine belongs to a class of cardiovascular drugs, which act at the voltage gated calcium channel of the CaV1, or L-type, class. Amlodipine also has antihypertensive and antianginal effects. Its activity resides mainly in the (-)-isomer. Amlodipine inhibits growth of human epidermoid carcinoma A431 cells and has antireproductive effects in male rats.
human ... CACNA1C(775), CACNA1D(776), CACNA1F(778), CACNA1S(779)
A8727 Antalarmin hydrochloride ≥98% (HPLC), solid Antalarmin hydrochloride is a non-peptide CRF1 corticotropin-releasing factor receptor antagonist.
Antalarmin serves as a non steroidal inhibitor of pregnancy even during the early stages. It is known to delay parturition. It also prevents the development of gastric ulcers which arises in response to stress.
A0487   Argatroban monohydrate ≥98% (HPLC) Argatroban is a potent, seletive, univalent direct inhibitor of thrombin. It directly inhibits thrombin by binding only to its active site (thus univalent) as compared to Bivalent DTIs (hirudin and analogs) which bind both to the active site and exosite 1.
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.
PZ0001 Atorvastatin calcium salt trihydrate ≥98% (HPLC) Atorvastatin calcium salt trihydrate is a specific inhibitor of HMG-CoA reductase. HMG-CoA reductase is the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early step in cholesterol biosynthesis. Atorvastatin is used in the treatment of hypercholesterolemia.
A0132 Atropine ≥99% (TLC), powder Atropine is used to treat myopia and ocular axial elongation in Asian children. Small dosage of atropine is used to slow down the heart rate.
Competitive nonselective antagonist at central and peripheral muscarinic acetylcholine receptors.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133), LOC730413(730413)
mouse ... Chrm1(12669)
rat ... Chrm1(25229), Chrm2(81645), Chrm3(24260), Drd2(24318), Htr1a(24473)
PZ0190 Avasimibe ≥98% (HPLC) Avasimibe (CI-1011) is an orally bioavailable Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) inhibitor. It was originally developed as an antilepic drug, and was shown to significantly reduce plasma total triglyceride and VLDL-cholesterol, but later clinical trials were disappointing. ACAT has also been investigated as a potential therapeutic target for Alzheimer′s disease. Recent studies have looked at the effects of avasimibe in reducing amyloid pathology by limiting generation and increasing clearance of diffusible amyloid-beta (Abeta).
PZ0123 Avridine ≥97% (HPLC) Avridine is a potent synthetic adjuvant that can induce arthritis in most rat strains; immunomodulator and interferon-inducing.
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.
human ... FLT1(2321), FLT4(2324), KDR(3791)
PZ0007 Azithromycin dihydrate ≥98% (HPLC) Azithromycin dihydrate is a macrolide antibiotic, azalide subclass. It binds to the 50S subunit of the 70S bacterial ribosomes and inhibits RNA-dependent protein synthesis in bacterial cells. Azithromycin also has anti-immunomodulatory/anti-inflammatory properties, which make it useful in treating cystic fibrosis.
Azithromycin is a non-β-lactam antibody, effective against infections associated with respiratory tract, skin, tissues and genital chlamydia. It also acts against Plasmodium falciparum and P. vivax, which are multidrug resistance species that transmit malaria. Azithromycin targets the ribosome and prevents protein synthesis. It is soluble in lipids and metabolizes in liver by undergoing demethylation.
PZ0018   Bazedoxifene acetate ≥98% (HPLC) Bazedoxifene is a third generation nonsteroidal selective estrogen receptor modulator (SERM), used clinically to treat postmenopausal osteoporosis. Bazedoxifene binds to estrogen receptor-α with IC50 = 26 nM, similar to that of raloxifene, but lower affinity than 17-β estradiol. Bazedoxifene did not stimulate proliferation of MCF-7 cells, instead inhibited 17β -estradiol-induced proliferation with IC50 = 0.19 nM, exhibiting a desirable profile of agonist/antagonist activity.
PZ0187 Begacestat ≥98% (HPLC) Begacestat (GSI-953) is a selective γ-secretase inhibitor that selectively inhibits cleavage of APP over Notch.
human ... APH1A(51107), APH1B(83464), NCSTN(23385), PSEN1(5663), PSEN2(5664), PSENEN(55851)
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.
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.
human ... ABL1(25), HCK(3055), LYN(4067), SRC(6714)
C0246 Cabergoline ≥98% (HPLC) Cabergoline, a lysergic acid amide derivative, is a potent dopamine D2 receptor agonist. It also acts on dopamine receptors in lactophilic hypothalamus cells to suppress prolactin production in the pituitary gland. It has been used for monotherapy of Parkinson′s disease in the early phase; combination therapy, together with levodopa and a decarboxylase inhibitor such as carbidopa, in progressive-phase Parkinson′s disease and adjunctive therapy of prolactin-producing pituitary gland tumors (microprolactinomas).
human ... DRD2(1813)
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.
Celecoxib is majorly bound to plasma proteins and is eliminated from liver via cytochrome P450 metabolic pathway. Celecoxib is recommended drug for the management of inflammation in osteoarthritis and rheumatoid arthritis. It may be effective in treating colorectal cancer in combination with chemoradiotherapy.
human ... PTGS2(5743)
C3618 Cetirizine dihydrochloride ≥98% (HPLC) Cetirizine hydrochloride is an orally active and selective H1-receptor antagonist. Antihistaminic; Piperazines. Non-sedating type histamine H1-receptor antagonist; major metabolite of hydroxyzine. Pharmacological activity resides primarily in the (R)-isomer.
Cetirizine is a racemic mixture of (R)-levocetirizine and (S)-dextrocetirizine. It exists as a zwitterion at acidic pH and gets absorbed by passive diffusion. Cetirizine is a prescribed drug for allergic rhinitis and chronic idiopathic urticaria.
human ... HRH1(3269)
C5874 Cidofovir hydrate ≥98% (HPLC) Selective inhibitor of viral DNA synthesis through the selective inhibition of viral DNA polymerase.
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.
PZ0136 CP-100263 dihydrochloride hydrate ≥97% (HPLC) CP-100263 is an NK-1 neurokinin receptor antagonist.
PZ0171 CP-100356 monohydrochloride >98% (HPLC) CP-100356 is a specific inhibitor of MDR1 (P-Gp), the protypical ABC transporter. The compound has low uM to nM potency for inhibiting several MDR-1 substrates (calcein-AM, digoxin) in transfected MDCKII cells. CP-100356 also inhibits prazosin transport in human breast cancer resistance protein (BCRP)-transfected MDCKII cells, suggesting that it acts as a dual inhibitor. CP-100356 does not inhibit multidrug resistance-associated protein 2 (MPR2 IC50 >15 mM).
PZ0107 CP-101537 ≥98% (HPLC) CP-101537 is a MMP inhibitor, candidate drug for myocardial infarction therapy, and antibacterial.
SML0053 CP-101,606 ≥98% (HPLC) CP-101,606 (Traxoprodil) plays a role in inhibiting glutamate-induced death in rats. It may exhibit therapeutic effects against human ischemia and neurodegenerative disorders. Traxoprodil is metabolized by cytochrome P450 (CYP) 2D6.
Traxoprodil (CP-101,606) is a potent noncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptors, selective for the NR2B subunit. It has been shown to be neuroprotective in animal models of brain injury and stroke.
human ... GRIN1(2902), GRIN2B(2904)
PZ0121 CP-135807 ≥98% (HPLC) CP-135807 is a selective 5-HT1D agonist.
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.
PZ0115 CP-31398 dihydrochloride hydrate ≥98% (HPLC) CP-31398 dihyrochloride hydrate is a p53 stabilizer; apoptosis inducer.
human ... TP53(7157)
mouse ... TP53(22059)
rat ... TP53(24842)
PZ0189 CP-316819 ≥98% (HPLC) CP-316819 belongs to the family of indole-2-carboxamide series of phosphorylase inhibitors. It has an ability to regulate interaction of glycogen targeting subunit (GL) 16mer peptide with phosphorylase a.
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.
PZ0137 CP-471474 ≥98% (HPLC) CP-471474 is a broad spectrum inhibitor of matrix metalloproteinases. CP-471474 has a low nM IC50 efficacy for MMP-2, MMP-3, MMP-9, and MMP-13. CP-471474 has low potency against MMP-1 (IC50 > 1 uM). CP-471474 prevents left ventricular remodeling after experimental myocardial infarction in mice. CP-471474 also inhibits cigarette smoke-induced lung inflammation and the progression of emphysema in guinea pig models.
PZ0125 CP-53631 ≥98% (HPLC) CP-53631 is a selective serotonin reuptake inhibitor (SSRI); antidepressant.
C1112 CP-55940 >98% (HPLC), powder CP-55940 is a nonclassical cannabinoids (NCCs), which lack the tetrahydropyran ring. CP-55940, a derivative of CP-47,497 is enantioselective. Due to its amphipathic nature, CP-55940 tethers in biological membrane making it favourable for the cannabinoid receptor interaction. CP-55940 belongs to the cyclohexylphenol category and modulates the brain lipidome leading to dysregulation especially during adolescence. It inhibits capsaicin-evoked sensitization of nociceptive and spinal dorsal horn neurons.
CP-55940 is a selective cannabinoid receptor agonist.
human ... CNR1(1268), CNR2(1269)
rat ... Cnr1(25248)
PZ0130 CP-64434 hydrate ≥98% (HPLC) CP-064434 is an antibiotic; anti-proliferative HDAC inhibitor.
PZ0124 CP-66713 ≥98% (HPLC) CP-66713 is an adenosine A2 receptor antagonist.
PZ0127   CP-74416 methanesulfonate hydrate ≥98% (HPLC) CP-74416 is a primary Danofloxacin metabolite. The compound belongs to a group of quinolone antibiotic. CP-74416 is an inhibitor of the bacterial DNA gyrase.
PZ0173 CP-775146 ≥98% (HPLC) CP-775146 is a potent and selective PPARα agonist.
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.
PZ0149 CP-868388 ≥98% (HPLC) CP-868388 is a potent PPARα agonist with a Ki of 10.8 nM.
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.
C9373 CP-96345 ≥98% (HPLC) CP-96345 is a selective NK1 antagonist. CP96345 inhibits substance P-induced salivation in the rat by classical in vivo bioassay, but did not inhibit NK2, NK3, or numerous other receptors.
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.
human ... ALK(238), MET(4233)
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.
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.
D6035   Disopyramide phosphate salt Class IA antiarrhythmic; sodium channel blocker
human ... SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
PZ0016 Dofetilide ≥98% (HPLC) Dofetilide is a Class III antiarrhythmic and hERG channel blocker. Dofetilide selectively blocks the rapid component of the delayed rectifier outward potassium current (IKr).
human ... KCNH2(3757)
D6821 Donepezil hydrochloride ≥98% (HPLC) Donepezil hydrochloride is a piperidine containing an organic compound and a non-competitive inhibitor. It is useful in treating Alzheimer′s disease, in which dementia is a prominent symptom. Donepezil is shown to induce cognitive ability and overall body function. It has a half-life of 70 hours.
Donepezil monohydrochloride monohydrate is a centrally acting reversible acetylcholinesterase inhibitor.
human ... ACHE(43)
D9815 Doxazosin mesylate ≥97% (HPLC), powder α1-adrenoceptor antagonist; relaxes smooth muscles of the prostate
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
rat ... Adra1a(29412), Adra1b(24173), Adra1d(29413)
PZ0140 EBPC ≥98% (HPLC) EBPC is an aldose reductase inhibitor; anti-cancer.
PZ0011 Eletriptan hydrobromide ≥98% (HPLC) Eletriptan hydrobromide is a serotonin 5-HT1B/1D receptor agonist; second generation anti-migraine drug.
human ... HTR1B(3351), HTR1D(3352), HTR1F(3355)
E6657 Eplerenone ≥98% (HPLC) Eplerenone is an aldosterone antagonist more specific for the mineralocorticoid receptor than spironolactone (S3378), having lower affinity for progesterone, androgen, and glucocorticoid receptors.
human ... NR3C2(4306)
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.
human ... ESR2(2100)
E5406 Ethopropazine hydrochloride ≥98% (HPLC), powder Ethoproprazine hydrochloride is an inhibitor of butyrylcholinesterase; antiparkinsonian. It reduces extrapyramidal motor effects, characteristic of Parkinson′s disease; also alleviates thermal hyperalgesia in rats.
human ... CHRM1(1128)
E7138 Ethosuximide Ethosuximide is an anticonvulsant drug and an antagonist for T-type calcium channel. It is known to prevent spike wave discharges, characterized in absence seizures.
human ... CACNA1G(8913), CACNA1H(8912), CACNA1I(8911)
PZ0006 Exemestane ≥98% (HPLC) Exemestane is a steroidal antiestrogen and irreversible aromatase inhibitor. Exemestane acts as a false substrate for the aromatase enzyme. Exemestane also prevents the conversion of androgens to estrogens and is used to treat estrogen-dependent breast cancer.
human ... CYP19A1(1588)
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.
human ... CYP1A2(1544)
G154 Gabapentin solid Anticonvulsant with unknown mechanism of action; crosses the blood brain barrier; increases GABA concentrations in the brain and reduces excitatory amino acid neurotransmission, perhaps through its effects on voltage-gated calcium channels; exhibits antinociceptive, anxiolytic, neuroprotective and anti-epileptic effects.
Gabapentin serves as a ligand for the α2δ subunit of L-type calcium channels.
human ... ADORA1(134), CACNA1A(773), CACNA1B(774), CACNA1C(775), CACNA1D(776), CACNA1E(777), CACNA1F(778), CACNA1G(8913), CACNA1H(8912), CACNA1I(8911), CACNA1S(779), CACNA2D1(781), CACNA2D2(9254), CACNA2D3(55799), CACNA2D4(93589), CACNB1(782), CACNB2(783), CACNB3(784), CACNB4(785), CACNG1(786), CACNG2(10369), CACNG3(10368), CACNG4(27092), CACNG5(27091), CACNG6(59285), CACNG7(59284), CACNG8(59283)
rat ... Cacna1a(25398)
G9518 Gemfibrozil Gemfibrozil selectively increases Apolipoprotein A-I levels. In yeast cells, application of gemfibrozil delays the start of DNA replication. It is used as a therapeutic agent for dyslipidemia.
human ... PPARA(5465)
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 Potassium inwardly-rectifying channel, subfamily J, member 1 (KCNJ1) plays a vital role in potassium balance. It is an ATP-dependent K+ channel blocker. The encoded protein is liable for the elimination of potassium in exchange for the absorption of sodium by the epithelial sodium channel (ENaC). Mutation in KCNJ1 is linked with several diseases, such as, antenatal Bartter syndrome and diabetes. Glipizide helps to repress the development of tumors and metastasis by preventing angiogenesis.
human ... ABCC8(6833), KCNJ1(3758), KCNJ11(3767)
I4883 Ibuprofen ≥98% (GC) Cyclooxygenase (COX) inhibitor that has greater activity against COX-1 than against COX-2.
human ... ALB(213), ALOX5(240), CYP1A2(1544), CYP2C9(1559), IL8RA(3577), PTGS1(5742), PTGS2(5743)
mouse ... Alox5(11689)
rat ... Alox5(25290), Ptgs1(24693)
I9910 Ibutilide hemifumarate salt ≥98% (HPLC) Ibutilide hemifumarate salt is considered a new generation "pure" Class III antiarrhythmic agent. Ibutilide binds to and alters the activity of hERG potassium channels, delayed inward rectifier potassium (IKr) channels and L-type (dihydropyridine sensitive) calcium channels.
human ... KCNH2(3757)
I7378 Indomethacin 98.5-100.5% (in accordance with BP) Cyclooxygenase (COX) inhibitor that is relatively selective for COX-1.
human ... ALB(213), ALOX5(240), ELA2(1991), GPR44(11251), IL1A(3552), PLA2G1B(5319), PTGDR(5729), PTGS1(5742), PTGS2(5743)
mouse ... Alox5(11689), Ptgdr(19214), Ptger1(19216), Ptger2(19217), Ptger3(19218), Ptger4(19219), Ptgs1(19224)
rat ... Alox5(25290), Ptgs1(24693), Ptgs2(29527)
K2753 (±)-Ketamine hydrochloride solid Selective NMDA glutamate receptor antagonist; veterinary anesthetic.
human ... GRIN1(2902), GRIN2A(2903), GRIN2B(2904), GRIN2C(2905), GRIN2D(2906), GRIN3A(116443), GRIN3B(116444)
K1884 S-(+)-Ketamine hydrochloride Selective NMDA glutamate receptor antagonist.
human ... GRIN1(2902), GRIN2A(2903), GRIN2B(2904), GRIN2C(2905), GRIN2D(2906), GRIN3A(116443), GRIN3B(116444)
L7795 Levocetirizine dihydrochloride ≥98% (HPLC) Levocetirizine hydrochloride is a nonsedating antihistamine. It is a histamine H1-receptor antagonist, the active isomer of cetirizine. Levocetirizine has high bioavailability, high affinity for and occupancy of the H1 receptor.
human ... HRH1(3269)
PZ0014 Linezolid ≥98% (HPLC) Linezolid is an oxazolidinone antimicrobial. It binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, thus inhibiting bacterial mRNA translation. Linezolid is also a weak, reversible, nonselective inhibitor of monoamine oxidase.
PZ0002 Maraviroc ≥98% (HPLC) Maraviroc is a CCR5 chemokine receptor antagonist, and antiretroviral entry inhibitor. Maraviroc inhibits HIV entry by blocking interaction of viral coat protein gp120 with the receptor.
Maraviroc is metabolised by cytochrome P450 3A4. The transport and absorption of maraviroc in the intestine and bile is regulated by P-glycoprotein (Pgp). Maraviroc binds to the active site pocket of chemokine receptor CCR5 making the receptor inactive.
human ... CCR5(1234)
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.
M4531 Meclofenamic acid sodium salt Cyclooxygenase (IC50 = 0.6 μM) and 5-lipoxygenase (IC50 = 46.3 μM) inhibitor.
Meclofenamic acid (MFA) is a nonsteroidal anti-inflammatory, analgesic and antipyretic drug. It inhibits prostaglandin biosynthesis pathway and finds its application in the treatment of postoperative and traumatic inflammation and swelling. MFA functions in opening the potassium voltage-gated channel subfamily Q member 2/member 3 (KCNQ2/Q3).
M1195 Metolazone ≥98% (HPLC), solid Inhibitor of thiazide-sensitive Na+-Cl- cotransporter; antihypertensive; moderate "loop" diuretic.
human ... SLC12A1(6557), SLC12A3(6559)
M6891 Mithramycin A from Streptomyces plicatus ≥90% (HPLC) Anticancer antibiotic. Inhibits transcription and protein synthesis. Binds to DNA in native chromatin. Substrate of Pgp in MDR phenotypes.
N7662 Nafarelin acetate salt hydrate ≥95% (HPLC), solid Nafarelin acetate salt hydrate is a gonadotrophin releasing hormone analogue and luteinizing hormone releasing hormone (LH-RH) agonist.
PZ0118 Nafoxidine hydrochloride ≥98% (HPLC) Nafoxidine is a potent estrogen receptor antagonist that exhibits anti-proliferative properties. It is a non-steroidal antiestrogen, a derivative of Tamoxifen.
PZ0013 Nelfinavir mesylate hydrate ≥98% (HPLC) Nelfinavir is a HIV protease inhibitor; antiretroviral; and anti-tumor agent.
Nelfinavir mesylate hydrate, also known as AG1343, is used as a therapeutic agent for acquired immunodeficiency syndrome (AIDS). It acts as an antifibrotic agent and is used to treat pulmonary fibrosis in patients with systemic sclerosis (SSc). In addition, nelfinavir mesylate hydrate reduces inflammation by activating protein phosphatase 2 (PP-2) and blocking mitogen-activated protein kinases (MAPK) signaling in macrophages. It also stimulate autophagy and exhibit anti-cancer property.
N7634 Nifedipine ≥98% (HPLC), powder Nifedipine is a L-type Ca2+ channel blocker; and induces apoptosis in human glioblastoma cells. Nifedipine has neuroprotection activity and protects substantia nigra. Nifedipine has antioxidant potential. Nifedipine downregulates inflammatory cytokines like macrophage inflammatory protein-2 (MIP-2), tumor necrosis factor-α (TNF-α). Nifedipine has antihypertensive properties. Nifedipine inhibits extracellular region of adenosine A2a receptor (ADORA2A) gene.
human ... ADORA2A(135), ADORA3(140), CACNA1C(775), CACNA1D(776), CACNA1F(778), CACNA1S(779), CACNA2D1(781), CYP1A2(1544), KCNH1(3756), TTR(7276)
mouse ... Cacna1c(12288)
rat ... Adora1(29290), Adora2a(25369), Cacna1c(24239), Cacna1d(29716), Kcnj1(24521), Kcnn4(65206), Tbxas1(24886)
PZ0177 OSU6162 hydrochloride ≥98% (HPLC) OSU6162 (PNU-96391) is a dopamine stabilizer, a drug that can stimulate or inhibit dopaminergic signaling depending on the dopaminergic tone. Dopaminergic stabilizers have been proposed to act as partial dopamine receptor agonists or as antagonists with both dopamine and behavioral stabilizing activity. Although affinity is not high (in vitro binding affinity for dopamine D2 receptor has a Ki of 447 nM), OSU6162 shows a high level of receptor occupancy.
O9637 Oxaprozin solid   human ... PTGIR(5739), PTGS1(5742), PTGS2(5743)
O5254 Oxazepam Anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
PZ0162 PD 0325901 ≥98% (HPLC) PD 0325901 by inhibiting mitogen-activated protein kinases (MAPKs) elicits growth-inhibitory and antiangiogenic effects on glioblastoma and melanoma tumor progression.
PD 0325901 is a potent MKK1 (MEK1) and MKK2 (MEK2) inhibitor. The Ki is 1.1 and 0.79 nM for MEK1 and MEK2, respectively. PD 0325901 was inactive against a panel of 27 other kinases. PD 0325901 inhibited C26 tumor pERK by 75% when dosed at 25 mg/kg in mice.
human ... MAP2K1(5604), MAP2K2(5605)
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.
P4620 PD 146176 ≥98% (HPLC), solid 15-Lipoxygenase inhibitor
human ... ALOX15(246)
mouse ... ALOX15(11687)
rat ... ALOX15(81639)
PZ0175 PD 149163 tetrahydrochloride hydrate ≥90% (HPLC) PD 149163 is a Neurotensin NTR1 receptor agonist; a Neurotensin (8-13) analog. PD149163 is a selective, brain penetrating NT1 receptor agonist with pro-cognitive, antipsychotic and anxiolytic effects.
PZ0141 PD-156707 ≥98% (HPLC) PD-156707 is a selective endothelin receptor (ETA) antagonist.
PZ0109 PD-161570 ≥98% (HPLC) PD-161570 is an inhibitor of human FGF-1 receptor tyrosine kinase.
PZ0144 PD-161989 2-Hydroxyethanesulfonate ≥98% (HPLC) PD-161989 is an AMPA receptor antagonist.
PZ0116 PD-166285 hydrate ≥98% (HPLC) PD-166285 hydrate is a broad spectrum protein tyrosine kinase inhibitor; Src and FGFR kinase inhibitor.
P0047 PD166793 hydrate ≥98% (HPLC) PD166793 is a broad spectrum, but class-selective, MMP inhibitor (low nM at MMP-2 & 3 and low μM at MMP-1, 7 & 9). Adding PD166793 to the high-fat diet substantially reduced the rise in blood glucose. The improvement of glucose homeostasis in PD166793-treated ZDF rats was a result of the enhancement of β-cell function. It prevents β-cell dysfunction and diabetes in female ZDF rats on a high-fat diet. It has been shown to block left ventricular remodeling and dysfunction in a rat model of heart failure. Preservation of normoglycemia and normal glucose tolerance in compound PD166793-treated animals is accompanied by preservation of the high serum insulin levels that are a consequence of the insulin resistance present in these animals. It is not reversing insulin resistance these animals. The most striking effect of the compound is on pancreatic insulin content and β-cell volume.
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.
PZ0113 PD173952 ≥98% (HPLC) PD173952 is a Src family kinase inhibitor.
PZ0142 PD-180970 ≥98% (HPLC) PD-180970 is a potent inhibitor of the p210 Bcr-Abl tyrosine kinase.
PZ0112 PD-184161 ≥98% (HPLC) PD-184161 is a MEK inhibitor.
PZ0181 PD184352 ≥98% (HPLC) PD184352 (CI-1040) is a highly selective non-competitive inhibitor of MEK (MKK1; MAPK kinase) and the closely related MKK2. It has anti-cancer activity, suppresses the ERK pathway, and has been used along with other classes of inhibitors to establish embryonic stem cell lines.
human ... MAP2K1(5604), MAP2K2(5605)
PZ0111 PD-407824 ≥98% (HPLC) PD-407824 is a Wee1/Chk1 inhibitor.
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.
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..
PZ0185 PF-431396 hydrate ≥98% (HPLC) PF-431396 is a potent inhibitor of PYK2 and FAK kinases (IC50 = 11 and 1.5 nM, respectively). PF-431396 increases bone formation and protects against bone loss in ovariectomized 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.
human ... RPS6KB1(6198)
mouse ... Rps6kb1(72508)
rat ... Rps6kb1(83840)
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.
PZ0117 PF-573228 ≥95% (HPLC) PF-573228 is a focal adhesion kinase (FAK) inhibitor; Non-receptor tyrosine kinase inhibitor.
PZ0151 PF-956980 hydrate ≥98% (HPLC) PF-956980 is a FGF1 receptor antagonist; PDGF receptor modulator; Flt3 tyrosine kinase modulator; and VEGF antagonist.
PZ0131 PF-998425 ≥98% (HPLC) PF-998425 is a novel, nonsteroidal androgen receptor antagonist.
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.
human ... CHRNA7(1139)
PZ0147 PHA-665752 hydrate ≥98% (HPLC) PHA-665752 ia a c-Met kinase inhibitor. PHA-665752 is ATP-competitive, an active-site inhibitor with greater than 50-fold selectivity for c-Met vs a panel of tyrosine and serine-threonine kinases.
PZ0178 PHA 767491 hydrochloride ≥98% (HPLC) PHA 767491 serves as a potential anticancer drug. It shows an ameliorating effect against acute myeloid leukemia, colon and breast cancer models. PHA 767491 possesses anti proliferating and apoptotic effect.
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.
P3029 Phencyclidine hydrochloride σ opioid receptor agonist and psychostimulant; inhibits NMDA glutamate receptor activation by binding to an allosteric site within the ion channel.
P6777 Phenelzine sulfate salt Non-selective MAO-A/B inhibitor.
human ... MAOA(4128), MAOB(4129)
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.
P0040 PP1 ≥98% (HPLC) PP1 is a potent and selective Src family protein tyrosine kinase inhibitor.
P0042 PP2 ≥98% (HPLC) PP2 is a selective inhibitor of Src-family tyrosine kinases with >10,000-fold selectivity over ZAP-70 and JAK2.
G6298   (RS)-PPG ≥98% (HPLC) (RS)-PPG is a potent selective group III mGluR agonist; anticonvulsant and neuroprotectant in vivo.
P3654 Prazepam Anxiolytic
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
P7791 Prazosin hydrochloride ≥99.0% (HPLC) Peripheral α1-adrenoceptor antagonist; vasodilator. Prazosin can be used to treat chronic posttraumatic stress disorder (PTSD). It plays a role in reducing blood pressure by relaxing blood vessels, hence used in the treatment of high blood pressure.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
PZ0010 Pregabalin ≥97% (NMR) Pregabalin is a lipophilic GABA analog/ligand at α2δ subunit of voltage-dependent Ca2+ channels. Pregabalin is an anticonvulsant, anxiolytic analgesic used to treat peripheral neuropathic pain and fibromyalgia.
human ... CACNA1A(773), CACNA1B(774), CACNA1C(775), CACNA1D(776), CACNA1E(777), CACNA1F(778), CACNA1G(8913), CACNA1H(8912), CACNA1I(8911), CACNA1S(779), CACNA2D1(781), CACNA2D2(9254), CACNA2D3(55799), CACNA2D4(93589), CACNB1(782), CACNB2(783), CACNB3(784), CACNB4(785), CACNG1(786), CACNG2(10369), CACNG3(10368), CACNG4(27092), CACNG5(27091), CACNG6(59285), CACNG7(59284), CACNG8(59283)
P9180 Procaterol hydrochloride β2-adrenoceptor agonist; bronchodilator.
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.
Q0632 Quinapril hydrochloride ≥98% (HPLC), solid Quinapril is a short-acting angiotensin converting enzyme (ACE) inhibitor.
human ... ACE(1636)
R0404 Ramipril ≥98% (HPLC) Angiotensin converting enzyme (ACE) inhibitor.
human ... ACE(1636)
R8781   Rapamycin Ready Made Solution, 2.5 mg/mL in DMSO (2.74 mM), from Streptomyces hygroscopicus Rapamycin is a macrocyclic triene antibiotic possessing potent immunosuppressant and anticancer activity. It forms a complex with FKBP12 that binds to and inhibits the molecular target of rapamycin (mTOR). mTOR is a member of the phosphoinositide kinase-related kinase (PIKK) family that enhances cellular proliferation via the phosphoinositol 3-kinase/Akt signaling pathway. Inhibition of this pathway by rapamycin blocks downstream elements that result in cell cycle arrest in G1. The effectors of mTOR action include 4EBP1 and S6K1.
R0395 Rapamycin from Streptomyces hygroscopicus ≥95% (HPLC), powder A macrocyclic triene antibiotic that binds to and inhibits the molecular target of rapamycin (mTOR). It forms a complex with FKBP12 that binds to and inhibits the molecular target of rapamycin (mTOR). Rapamycin is a potent immunosuppressant and has anticancer activity.
human ... FKBP1A(2280)
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.
PZ0132 SC-51322 ≥98% (HPLC) SC-51322 is a selective EP1 prostanoid receptor antagonist.
PZ0110 SC-57461A ≥98% (HPLC) SC-57461A is an inhibitor of leukotriene A4 hydrolase.
PZ0139 SC-58125 ≥98% (HPLC) SC-58125 is a selective cyclooxygenase 2 (COX-2) inhibitor.
S6319 Sertraline hydrochloride ≥98% (HPLC) Selective serotonin reuptake inhibitor, antidepressant.
Sertraline suppresses platelet function and exhibits antiplatelet and endothelium protective functions. It relieves depression and improves the quality of life in patients with cardiovascular disorders. It can also be prescribed to treat depression in Parkinson′s disease.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363), SLC6A4(6532)
PZ0003 Sildenafil citrate salt ≥98% (HPLC) Sildenafil is a potent, selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5). Sildenafil is used to treat erectile dysfunction and pulmonary arterial hypertension. NO activates guanylate cyclase, which results in increased levels of cGMP, producing smooth muscle relaxation. Sildenafil enhances the effect of NO by inhibiting PDE5, which is responsible for degradation of cGMP.
human ... PDE5A(8654)
PZ0174 Sonepiprazole hydrate ≥98% (HPLC) Sonepiprazole (U-101387) is a selective D4 dopamine antagonist. Ki = 10 nM for the dopamine D4.2 receptor.
S7701 Sorbinil ≥98% (HPLC) Sorbinil decreases the level of sorbitol in red blood cells and increases the velocity of nerve conduction. It maintains the myo-inositol content in the nerve and prevents the reduction of sodium-potassium ATPase activity. This action is beneficial in providing symptomatic relief in patients with diabetic neuropathy.1,2
Sorbinil is an inhibitor of Aldose Reductase (AR). AR family members AKR1B1 and AKR1B10 have additionally been shown to play roles in inflammation and cancer.
S3378 Spironolactone 97.0-103.0% Spironolactone is a competitive aldosterone receptor antagonist. Used as potassium sparing diuretic.
Spironolactone reduces aldosterone-induced potassium/magnesium loss and myocardial fibrosis. It reduces hypertension, improves the endothelial function and reduces the overall morbidity and mortality in patients with chronic heart failure. Spironolactone improves nitric oxide bioactivity and vascular endothelial vasodilator dysfunction.
human ... HSD17B1(3292), NR3C2(4306)
rat ... Ar(24208)
S0130 Streptozocin ≥75% α-anomer basis, ≥98% (HPLC), powder An N-nitroso-containing compound that acts as a nitric oxide donor in pancreatic islets; induces death of insulin-secreting cells, producing an animal model of diabetes. Potent DNA methylating agent that induces chromosomal breakage. Cytotoxic to neuroendocrine tumor cell lines that express the GLUT2 glucose transporter.
Clinically, the chemical is used for the treatment of pancreatic β cell carcinoma.
S8442 SU 5416 ≥98% (HPLC) SU 516 inhibits the activity of neuronal nitric oxide synthase and protects the neuronal cells from nitric oxide-mediated neurotoxicity.1 It also acts an agonist of aryl hydrocarbon receptor and is an effective clinical agent for treating autoimmune diseases and transplant rejection.2
SU 5416 is a vascular endothelial growth factor (VEGF) receptor protein tyrosine kinase 1/2 inhibitor.
human ... EGFR(1956), FLT1(2321), IGFBP1(3484), IL2(3558), KDR(3791), PDGFRB(5159)
mouse ... Flt1(14254), Kdr(16542)
PZ0150 SU5614 ≥98% (HPLC) SU5614 is a FMS-like tyrosine kinase 3 (FLT3) inhibitor; selective inhibitor of VEGF and PDGF receptor tyrosine kinases.
PZ0012 Sunitinib malate ≥98% (HPLC) Sunitinib has greater bioavailability and potency compared to other inhibitors. It prevents angiogenesis.
Sunitinib malate is a receptor tyrosine kinase inhibitor, which targets VEGF-R1, VEGF-R2, VEGF-R3, PDGF-Rα, PDGF-Rβ, KIT, FLT3, CSF-1R, and RET. Sunitinib malate is an anticancer drug.
human ... CSF1R(1436), FLT1(2321), FLT3(2322), FLT4(2324), KDR(3791), KIT(3815), PDGFRA(5156), PDGFRB(5159), RET(5979)
PZ0020 Temsirolimus ≥98% (HPLC) Temsirolimus is a specific inhibitor of mammalian target of rapamycin (mTOR) mTOR Complex 1 (mTORC1). Temsirolimus is an antiproliferative and antiangiogenic, the first-in-class mTOR inhibitor approved for the treatment of patients with advanced poor prognosis renal cell carcinoma.
The inhibitory action of temsirolimus is mediated by FKBP-12 (FK506-binding protein 12), a major intracellular protein. It is useful in treating renal-cell carcinoma.
human ... FKBP1A(2280)
PZ0021 Tigecycline hydrate ≥98% (HPLC) Tigecycline is a broad spectrum glycylcycline antibiotic. Tigecycline is bacteriostatic, that inhibits protein synthesis by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline is active against resistant strains of gram-positive and gram-negative bacteria, avoiding the two most common mechanisms of resistance to the tetracycline antimicrobials: tetracycline efflux pump proteins and ribosomal protection proteins.
PZ0009 Tolterodine L-tartrate ≥98% (HPLC) Tolterodine L-tartrate is a bladder-specific muscarinic antagonist.
PZ0170 Torcetrapib ≥98% (HPLC) Torcetrapib is a Cholesteryl ester transfer protein (CETP) inhibitor. CETP normally transfers cholesterol from HDL cholesterol to very low density or low density lipoproteins (VLDL or LDL). Inhibition of this process results in higher HDL levels (the "good" cholesterol-containing particle) and reduces LDL levels (the "bad" cholesterol). Unfortunately clinical trials were stopped because of excessive all cause mortality. Reasons are still being investigated, but may be related to some off target effects such as an increase in aldosterone secretion not found in some other CETP inhibitors.
T2573 Troglitazone ≥98% (HPLC) PPARγ agonist; anti-diabetic thiazolidinedione (TZD) with anti-inflammatory and anti-tumor activity; induces apoptosis via a p53 pathway.
human ... PPARA(5465), PPARG(5468)
PZ0015 Trovafloxacin mesylate >98% (HPLC) Trovafloxacin mesylate acts as a pannexin1 (Panx1) inhibitor.
Trovafloxacin mesylate is a broad spectrum antibiotic. Trovafloxacin mesylate blocks the activity of DNA gyrase and topoisomerase IV, enzymes essential in the repliction, transcription, and repair of bacterial DNA.
PZ0152 UK-356618 ≥98% (HPLC) UK-356,618 is a potent, selective inhibitor of Matrix metalloproteinase MMP3 (stromelysin-1). MMP-3 IC50 = 5.9 nM, selectivity is 140-fold vs MMP-1, -2, -9, and -14.
PZ0156 UK-383,367 ≥98% (HPLC) UK-383,367 is a procollagen C-proteinase (PCP) inhibitor.
PZ0160 UK-5099 ≥98% (HPLC) UK-5099 induces lactate generation.
UK-5099 is a potent inhibitor of the mitochondrial pyruvate transporter. In rat heart mitochondria, UK-5099 inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.
U3885 UK-78282 monohydrochloride ≥98% (HPLC) UK-78282 blocks both Kv1.3 and Kv1.4. Kv1.3 and Kv1.4 are members of the Shaker family of voltage-gated potassium channels. Kv1.3 is expressed in brain and in effector memory T (Tem) cells, and Kv1.4 is expressed in brain. Both channels are involved in setting the membrane potential of neurons. In addition, Kv1.3 maintains the membrane potential for T memory cells and is up-regulated upon T cell activation, contributing to multiple immune processes and disorders. Blockers of Kv1.3 have long been sought for therapeutic benefit, and they are also valuable tools for studying the immune system. Selective blockers of Kv1.4 are desired, as there are few if any currently available. UK-78282 is valuable for immune system studies, where the absence of Kv1.4 makes it functionally selective for Kv1.3, and it has shown suppression of T cell activation. UK-78282 is also valuable for the study of Kv1.4 function.
PZ0179 Valdecoxib ≥98% (HPLC) Valdecoxib is a non-steroidal anti-inflammatory drug (NSAID), a cyclooxygenase-2 (COX-2) selective inhibitor.
human ... PTGS2(5743)
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.
V4629 (±)-Verapamil hydrochloride ≥99% (titration), powder α1-adrenoceptor antagonist; L-type calcium channel blocker. Blocks L-type Ca2+ channels in smooth and cardiac muscle, induces apoptosis of human primary and metastatic colon adenocarcinoma cells in vitro. Drug resistance reversal agent acting on Pgp, e.g. decrease renal tubule elimination of digoxin. Increases basal ATPase activity of Pgp. Substrate of Cyp3A4 and CYP2C6.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), CACNA1C(775), CACNA1D(776), CACNA1F(778), CACNA1S(779)
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.
Voriconazole is used to treat invasive aspergillosis (IA). It is vigorous against Candida species, including the strains of Candida albicans, which shows resistance to fluconazole.
Z2777 Ziprasidone hydrochloride monohydrate ≥98% (HPLC), solid Ziprasidone is an atypical antipsychotic; FDA approved for the treatment of schizophrenia.
human ... DRD2(1813), HTR2A(3356), HTR2C(3358)
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.
Z4527 Zopolrestat ≥98% (HPLC) Zopolrestat is an inhibitor of Aldose Reductase. AR family members AKR1B1 and AKR1B10 have additionally been shown to play roles in inflammation and cancer.