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