Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides and has potential roles in obesity, diabetes, and atherosclerosis. PF-04620110 is a potent inhibitor of DGAT-1 (IC50 = 19 nM) that is without effect on DGAT-2. It has high oral bioavailability (100%) in rats, with a moderate half-life of 6.8 hours. PF-04620110 significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.
