Purity >95%. Diacylglycerol acyltransferases (DGATs) catalyze the final step in triglyceride synthesis. DGAT-1 deficient mice demonstrate a phenotype that is protective against the development of diet-induced obesity (DIO) or insulin resistance, implicating the actions of this enzyme in the development of such metabolic disorders. A-922500 is a potent orally active inhibitor of DGAT-1 activity, inhibiting both human and mouse forms of the enzymes with IC50 values of 7 and 24 nM, respectively. When administered at 3 mg/kg to DIO mice, A-922500 conferred significant weight loss within seven days without affecting food intake and significantly reduced plasma and liver triglycerides with chronic dosing. A-922500 does not inhibit DGAT-2, ACAT-1, or ACAT-2.