Metabolism Standards

Tetroxoprim (Standard) is the analytical standard of Tetroxoprim. This product is intended for research and analytical applications. Tetroxoprim is an antimicrobial DHFR inhibitor.

Muzolimine (Standard) is the analytical standard of Muzolimine. This product is intended for research and analytical applications. Muzolimine (BAY-g 282) is a slow and long lasting diuresis agent. Muzolimine produces a diuresis in the loop of Henle and also shows anti-hypertensive and natriuresis effects. Muzolimine can be used for the research of cardiovascular disease.

Tiaprofenic acid (Standard) is the analytical standard of Tiaprofenic acid. This product is intended for research and analytical applications. Tiaprofenic acid is an orally active nonsteroidal anti-inflammatory agent (NSAID) with anti-inflammatory and analgesic potency. Tiaprofenic acid inhibits prostaglandin synthesis by suppressing cyclo-oxygenase (COX). Tiaprofenic acid can be used in the treatment of rheumatic diseases.

Cibenzoline (Standard) is the analytical standard of Cibenzoline. This product is intended for research and analytical applications. Cibenzoline is a class Ia antiarrhythmic active molecule with low anticholinergic activity. Cibenzoline is a K_ATP channel inhibitor, acting through the pore forming subunit Kir6.2, with an IC₅₀ of 22.2 μM. Cibenzoline inhibits I_Kr and I_Ks currents with IC₅₀ values of 8.8 μM and 12.3 μM, respectively. Cibenzoline is used in the study of cardiac diseases. In addition, Cibenzoline can induce hypoglycemia.

Devazepide (Standard) is the analytical standard of Devazepide. This product is intended for research and analytical applications. Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC₅₀s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders.

Ketanserin (Standard) is the analytical standard of Ketanserin. This product is intended for research and analytical applications. Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (I_hERG) in a concentration-dependent manner (IC₅₀=0.11 μM).

Tenidap (Standard) is the analytical standard of Tenidap. This product is intended for research and analytical applications. Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC₅₀ values of 0.03 μM and 1.2 μM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties. Tenidap is also a specific SLC26A3 inhibitor.

Cobicistat (Standard) is the analytical standard of Cobicistat. This product is intended for research and analytical applications. Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC₅₀s of 30-285 nM. Cobicistat is a pharmacokinetic enhancer which increases the overall absorption of several HIV medications.

Canagliflozin (Standard) is the analytical standard of Canagliflozin. This product is intended for research and analytical applications. Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC₅₀s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.

Vismodegib (Standard) is the analytical standard of Vismodegib. This product is intended for research and analytical applications. Vismodegib (GDC-0449) is a BBB-permeable and orally active hedgehog pathway inhibitor with an IC₅₀ of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC₅₀ values of 3.0 μM and 1.4 μM, respectively.

Sotrastaurin (Standard) is the analytical standard of Sotrastaurin. This product is intended for research and analytical applications. Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with K_is of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.

Brivanib (Standard) is the analytical standard of Brivanib. This product is intended for research and analytical applications. Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC₅₀ of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β.

Regorafenib (Standard) is the analytical standard of Regorafenib. This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC₅₀ values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.

Zotepine (Standard) is the analytical standard of Zotepine. This product is intended for research and analytical applications. Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT_2A, 5-HT_2C, Histamine H₁, α₁-adrenergic and Dopamine D₂ receptors, with K_ds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo.

Saxagliptin (Standard) is the analytical standard of Saxagliptin. This product is intended for research and analytical applications. Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (K_i = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research.

Linagliptin (Standard) is the analytical standard of Linagliptin. This product is intended for research and analytical applications. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC₅₀ of 1 nM.

Masitinib (Standard) is the analytical standard of Masitinib. This product is intended for research and analytical applications. Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC₅₀=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC₅₀s=540/800 nM), Lyn (IC₅₀= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity.

Pazopanib (Standard) is the analytical standard of Pazopanib. This product is intended for research and analytical applications. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC₅₀s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

Cediranib (Standard) is the analytical standard of Cediranib. This product is intended for research and analytical applications. Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC₅₀s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.

Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC₅₀s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2.