PF-06471553 is a potent and selective Monoacylglycerol acyltransferase 3 (MGAT3) inhibitor. PF-06471553 selectively inhibits MGAT3 with high in vitro potency and cell efficacy. In the presence of a combination of diacylglycerol acyltransferases 1 and 2 (DGAT1 and DGAT2) inhibitors, an oral administration of PF-06471553 exhibited inhibition of the incorporation of deuterium-labeled glycerol into TAG in mouse model. Inhibition of triacylglycerol (TAG) biosynthetic enzymes has been suggested as a promising strategy to treat insulin resistance, diabetes, dyslipidemia, and hepatic steatosis.
