PF-06424439

PF-06424439 is an orally bioavailable inhibitor of diacylglycerol acyltransferase 2 (DGAT-2, IC50 = 14 nM). It is selective for DGAT-2 over the related acyltransferases DGAT-1, MGAT-2, and MGAT-3 (IC50s = >50 µM). PF-06424439 (0.1-10 mg/kg) reduces plasma triglyceride levels in sucrose-fed rats in a dose-dependent manner. It also reduces plasma levels of cholesterol and triglycerides as well as hepatic triglycerides in LDL receptor knockout mice fed a high-fat, high-cholesterol diet when administered at a dose of 60 mg/kg per day.Formal Name: [(3R)-1-[2-[1-(4-chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone, monomethanesulfonate. CAS Number: 1469284-79-4. Molecular Formula: C22H26ClN7O . CH3SO3H. Formula Weight: 536.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble, Water: soluble. SMILES: O=C(N1CCCC1)[C@@H]2CCCN(C3=NC(N=C(C4(CC4)N5N=CC(Cl)=C5)N6)=C6C=C3)C2.OS(C)(=O)=O. InChi Code: InChI=1S/C22H26ClN7O.CH4O3S/c23-16-12-24-30(14-16)22(7-8-22)21-25-17-5-6-18(26-19(17)27-21)29-11-3-4-15(13-29)20(31)28-9-1-2-10-28,1-5(2,3)4/h5-6,12,14-15H,1-4,7-11,13H2,(H,25,26,27),1H3,(H,2,3,4)/t15-,/m1./s1. InChi Key: ZSTFDNQQOJUJFL-XFULWGLBSA-N.