[(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate

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.

PF-06424439 has been used as a diacylglycerol acyltransferase 2 (DGAT2)?inhibitor:

• to study its effects on cell mortality and lipid synthesis in epithelial colon cells and colorectal cancer stem cells
• to study its effects on HeLa cells
• to study its inhibitory effects on neutral lipid synthesis in HT-1080 cells

PF-06424439 is a potent and selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).

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