An orally bioavailable inhibitor of DGAT-2 (IC50 = 14 nM); selective for DGAT-2 over the related acyltransferases DGAT-1, MGAT-2, and MGAT-3 (IC50s = >50 μM); reduces plasma triglyceride levels in sucrose-fed rats in a dose-dependent manner from 0.1-10 mg/kg; reduces plasma levels of cholesterol and triglycerides as well as hepatic triglycerides in LDL receptor knockout mice fed a high-fat, high-cholesterol diet at 60 mg/kg per day