Therapeutics: Diacylglycerol O-acyltransferase-2 (DGAT2)

In vitro and mouse studies identified a DGAT2 inhibitor that could help treat hypercholesterolemia. Chemical synthesis and testing in DGAT2 activity assays of imidazopyridine analogs identified a compound that inhibited DGAT2 with an IC50 of 14 nM. In a mouse model of hypercholesterolemia, the compound decreased serum levels of cholesterol and triglycerides compared with vehicle. Next steps could include testing the compound in additional animal models of hypercholesterolemia...