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SML0074 Acenocoumarol ≥98% (HPLC) Acenocoumarol is a warfarin analog, an anticoagulant that inhibits Vitamin K epoxide reductase. This results in depletion of the reduced form of vitamin K (vitamin KH2), limiting the gamma-carboxylation and subsequent activation of the vitamin K-dependent coagulation factors II, VII, IX, and X and anticoagulant proteins C and S, resulting in decreased prothrombin levels and the amount of thrombin generated.
 
A9657 DL-Aminoglutethimide DL-Aminoglutethimide is a derivative of the sedative glutethimide. Originally introduced as an anticonvulsant, it was found to cause adrenal insufficiency. Blocks adrenal steroidogenesis by inhibiting the enzymatic conversion of cholesterol to pregnenolone. It also blocks the peripheral conversion (aromatization) of androgenic precursors to estrogens. The D-isomer is 30 times more potent at inhibiting aromatase activity, whereas the L-isomer is more potent at inhibiting cholesterol side-chain cleavage (steroidogenesis).
human ... CYP17A1(1586), CYP19A1(1588)
rat ... Cyp19a1(25147)
A9899 Antazoline hydrochloride Imidazoline agonist; more potent than efaroxan in inducing insulin release from β cells; H1 histamine receptor antagonist.
human ... HRH1(3269)
A9361 Artemether ≥98% (HPLC) Artemether is a methyl ether derivative of artemisinin. It is used against multi-drug resistant strains of the malaria parasite, Plasmodium falciparum, and shows potential in treatment of schistosomiasis.
 
B0935 Benazepril hydrochloride ≥98% (HPLC), solid Benazepril is a long-acting angiotensin converting enzyme (ACE) inhibitor.
 
B5683 Betaxolol hydrochloride >98% (HPLC) Selective β1 adrenoceptor antagonist.
human ... ADRB1(153)
B1680   Bradyzide di(trifluoroacetate) salt hydrate ≥98% Potent, orally active, non-peptide B2 bradykinin receptor antagonist.
 
SML0057 Camostat mesylate ≥98% (HPLC) Camostat is a synthetic, orally bioavailble serine protease inhibitor.
Camostat mesylate inhibits the production of TNF-α and monocyte chemoattractant protein-1 (MCP-1) by monocytes. It also inhibits the activity of pancreatic stellate cells. Camostat mesylate regulates the cytokine expression and inflammation and is effective in the treatment of dibutyltin dichloride-induced rat pancreatic fibrosis.
 
C4024 Carbamazepine powder Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site. Sodium channel inhibitor.
human ... BZRAP1(9256), GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), PRNP(5621), SCN5A(6331)
rat ... Scn2a1(24766), Scnn1a(25122), Scnn1g(24768), Slc6a1(79212)
C0987 CGP-13501 ≥98% (HPLC), solid Positive allosteric modulator of GABAB receptors.
human ... GABBR1(2550), GABBR2(9568)
C5851 CGP 35348 hydrate ≥97% (NMR), solid CGP 35348 hydrate is a GABAB-receptor antagonist.
 
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.
 
C8895 Clofazimine    
C7291 Clomipramine hydrochloride ≥98% (HPLC), powder Tricyclic antidepressant; inhibits serotonin and norepinephrine transporters.
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)
C6305 Clozapine Atypical antipsychotic compound. Selective antagonist for D4-dopamine receptor. Antagonist at 5-HT2A, 5-HT2C, 5-HT3, 5-HT6, and 5-HT7 serotonin receptors.
human ... ADRA1A(148), ADRA2A(150), ADRA2C(152), CHRM1(1128), DRD2(1813), DRD3(1814), DRD4(1815), HRH1(3269), HRH4(59340), HTR2A(3356), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR6(3362), HTR7(3363), KCNH1(3756), KCNH2(3757), UGT1A4(54657)
rat ... Adra1a(29412), Adra2a(25083), Adrb1(24925), Chrm1(25229), Drd1a(24316), Drd2(24318), Drd3(29238), Drd4(25432), Hrh1(24448), Htr1a(24473), Htr1b(25075), Htr2a(29595), Htr2b(29581), Htr2c(25187), Htr3a(79246), Htr7(65032), Slc6a4(25553)
C3662 Cyclosporin A from Tolypocladium inflatum, ≥95% (HPLC), solid A fungal metabolite possessing potent immunosuppressive properties. It inhibits the T-cell receptor signal transduction pathway via the formation of cyclosporin A−cyclophilin complex that inhibits calcineurin (protein phosphatase 2B). Inhibits nitric oxide synthesis induced by interleukin 1α, lipopolysaccharides and TNFα. Can block cytochrome c release from mitochondria.
human ... PPP3CA(5530), PPP3CB(5532), PPP3CC(5533), PPP3R1(5534), PPP3R2(5535)
D6899 Diclofenac sodium salt Diclofenac sodium salt is a nonsteroidal anti-inflammatory drug (NSAID) that acts as a competitive and irreversible inhibitor of prostaglandin synthetase. Its analgesic and anti-inflammatory activities are based on the prevention of the synthesis of arachinodate metabolites via cyclooxygenase inhibition. It is found to hinder the conversion of arachidonic acid to prostaglandins, which mediate inflammatory process. The NSAIDs are found to inhibit both cyclooxygenase enzymes, COX-1 and COX-2, causing undesirable gastrointestinal effect. Diclofenac sodium also functions as a scavenger of free radicals and serves a radioprotective role in restoring supercoiled form of plasmid DNA damaged by radiation back to normal. Diclofenac sodium is oxidized by the donation of electron and transfer of hydrogen atom. It can be a potential radioprotective agent.
Standard NSAID and cyclooxygenase (COX) inhibitor. Major metabolites are 4´-hydroxydiclofenac and 5´-hydroxydiclofenac. Has been used as substrate selective for CYP2C9.
human ... PTGS1(5742)
E1001 Ethisterone ≥99% (HPLC)    
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.
 
SML0038 Fluvastatin sodium hydrate ≥98% (HPLC) Fluvastatin is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Fluvastatin is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.
 
F9552 Formoterol fumarate dihydrate >98% (HPLC) β2-Adrenoreceptor agonist.
human ... ADRB2(154)
SML0029 Glycopyrrolate ≥98% (HPLC) Glycopyrrolate is long-acting muscarinic antagonist (LAMA). It is kinetically selective muscarinic M3 receptor antagonist.
 
I7379 Imipramine hydrochloride ≥99% (TLC) Tricyclic antidepressant; inhibits the serotonin and norepinephrine transporters with Kis of 7.7 nM and 67 nM, respectively. Has little effect on the dopamine transporter (Ki = 25 μM).
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)
I6658 Isradipine ≥98% (HPLC), solid L-type calcium channel blocker (also referred to as dihydropyridine-type calcium channel blocker); antihypertensive.
human ... CACNA2D1(781)
K2628   Ketotifen fumarate salt H1 histamine receptor antagonist.
human ... HRH1(3269), PDE7B(27115)
L8533 Lansoprazole ≥98% (TLC), powder Gastric proton pump inhibitor.
 
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.
 
L5420 Lumefantrine Lumefantrine is is an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.
 
M9651 Maprotiline hydrochloride >99% (HPLC), powder Selective norepinephrine uptake inhibitor.
 
M0267 (±)-Methadone hydrochloride powder, ≥98% (TLC) μ opioid receptor agonist that desensitizes both the μ opioid receptor and the δ opioid receptor on chronic exposure; narcotic analgesic, characterized by a gradual onset of action and prolonged, milder withdrawal; may also block L-type calcium channels independently of its effects on opioid receptors.
 
M137 Methysergide maleate salt solid Nonselective 5-HT1, 5-HT2, and 5-HT7 serotonin receptor antagonist; antimigraine.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR7(3363)
M5391 (±)-Metoprolol (+)-tartrate salt ≥98% (titration), powder β1-adrenoceptor antagonist.
human ... ADRB1(153)
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.
 
SML0195 Mifamurtide ≥98% (HPLC) Mifamurtide (Muramyl tripeptide phosphatidylethanolamine; MTP-cephalin; MTP-PE) is a synthetic, lipophilic analog of muramyl dipeptide. It acts as an immunostimulant promoting cancer cell destruction via in vivo macrophage activation.
Mifamurtide is an immunomodulator and regulates the activation of monocytes and macrophages. Mifamurtide upregulates the secretion of pro-inflammatory cytokines such as TNF-α, IL-1, IL-8, nitric oxide and prostaglandins E2 and D2. It has anti-tumor effects in children and young adults with high-grade osteosarcoma.
 
M5255 Mycophenolic acid ≥98% Mode of Action: This product acts by suppressing the cytokine-induced nitric oxide production, inhibiting early stage biosynthesis of purine nucleotides and as a specific inhibitor of IMP dehydrogenase.
human ... IMPDH1(3614), IMPDH2(3615)
N3136 Naltrexone hydrochloride Competitive antagonist for μ, κ, δ, and σ-opioid receptors; has greater oral efficacy and longer duration of action than naloxone.
human ... OPRD1(4985), OPRK1(4986), OPRM1(4988), OPRS1(10280)
N3538 Nateglinide ≥98% (HPLC), solid Nateglinide is a Kir6.2/SUR1 channel inhibitor and antidiabetic. It is selective for the SUR1 subtype, which is found on pancreatic islet cells. Nateglinide evokes KATP channel-dependent insulin secretion (50-200 μM) in the absence and presence of insulin.
 
N9289 NVP-231 ≥98% (HPLC) Ceramide kinase presents an attractive target for drug development because of its involvement in cell growth and inflammation. CerK biology is still poorly understood thus discovery and availability of inhibitors will facilitate research at this area. NVP-231 is a newly discovered potent, specific and reversible CerK inhibitor that competitively inhibits binding of ceraminde to CerK.
 
O3764 Oxcarbazepine ≥98% (HPLC), solid Anticonvulsant, antineuralgic. Inhibits veratrine-induced transmitter release.
rat ... Scnn1g(24768)
P2371 Pamidronate disodium salt hydrate ≥95% (NMR), solid Bone resorption inhibitor; inhibitor of farnesyl diphosphate synthase (IC50 = 200 nM).
 
P0021 Pantoprazole sodium hydrate ≥98% (HPLC) Pantoprazole is a gastric proton pump inhibitor.
 
P7547 Phentolamine hydrochloride ≥98% (TLC), powder α-adrenoceptor antagonist; peripheral vasodilator.
 
P7561 Phentolamine methanesulfonate salt ≥98% (TLC), powder α-Adrenergic receptor antagonist; peripheral vasodilator.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)
P0778 Pindolol ≥98% (TLC), powder β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator.
human ... ADRB1(153), HTR1A(3350)
P152 S(–)-Pindolol solid β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator. Active enantiomer of pindolol.
human ... ADRB1(153), HTR1A(3350), HTR1B(3351)
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.
 
R8404 Rufinamide ≥98% (HPLC), powder Broad-spectrum anticonvulsant.
 
S9318 Sandoz 58-035 >98% (HPLC), powder Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor.
Sandoz 58-035 inhibits the accumulation of cholesteryl esters and inhibits the esterification of cholesterol by 95% in arterial smooth muscle cells in culture.1 It does not affect the triglyceride metabolism by the gut.2
human ... SOAT1(6646)
rat ... Soat1(81782)
S2951 Stauprimide ≥98% (HPLC) Stauprimide is an enhancer stem cell differentiation into endoderm. In vitro differentiation of embryonic stem cells is of great interest to regenerative medicine, and current protocols are labor-intensive and expensive. Small molecules that induce or enhance differentiation are highly desired. High-content screening identified compounds that enhance endodermal differentiation in the presence of low levels of Activin A. Stauprimide increased definitive endodermal markers but not markers for visceral/parietal endoderm or mesoderm. Stauprimide-differentiated cells could be further differentiated into hepatocytes. Stauprimide treatment during differentiation decreased the concentration of Activin A required for definitive endoderm formation, and it eliminated the need for serum. The mechanism of action of stauprimide is to sensitize cells for differentiation. Stauprimide enabled differentiation into other cell lineages under varying differentiation conditions, including neurons, hematopoietic mesoderm, beating cardiac myocytes, and skeletal muscle. The cellular target of stauprimide was determined to be inhibition of NME2 transcription factor translocation to the nucleus, leading to down-regulation of c-Myc expression.
 
S8251 Succinylcholine chloride dihydrate 98.0-102.0%, solid Cholinergic antagonist which induces a long-lasting depolarization of the acetylcholine neuron membrane; neuromuscular blocking agent.
Succinylcholine is a cholinergic antagonist and a neuromuscular blocking agent. It induces depolarization of acetylcholine receptors on the muscle membrane and efflux of potassium from the muscle that leads to hypokalemia in individuals with upregulated expression of acetylcholine receptors.3
 
T2528 Terbutaline hemisulfate salt Terbutaline is a β-adrenoceptor agonist and is known to function as a bronchodilator. Studies have reported that terbutaline is potent inhibitor of premature labor6.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
T4264 Tetrahydrozoline hydrochloride ≥98% α-adrenoceptor agonist; imidazoline binding site ligand; vasoconstrictor.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)
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.
 
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.
human ... CHRNA3(1136), CHRNA4(1137), CHRNB2(1141), CHRNB4(1143), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242)
rat ... Chrna7(25302), Drd2(24318), Htr1a(24473), Htr3a(79246)
SML0142 Valsartan ≥98% (HPLC) Valsartan is an Angiotensin II type 1 (AT1) receptor antagonist and anti-hypertensive. Valsartan renders protection against heart attack and stroke resulting from abrupt increase in blood pressure. Valsartan reduces myocardial-infarction-related complications in heart attack survivors.
 
W1020 W146 hydrate ≥98% (HPLC) Potent S1P(1) competitive antagonist; Ki = 10-77 nM.
 
X6000 Xylometazoline hydrochloride α-adrenoceptor agonist; imidazoline binding site ligand.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)