T863 is a potent and selective, cell-permeable DGAT1 inhibitor that binds to the oleoyl-CoA binding pocket of DGAT1 with IC50 of 17 nM in TLC assay.
T863 shows no inhibitory activity against hMGAT3, hDGAT2, and hMGAT2 at >10 uM.
T863 inhibits DGAT1-mediated triacylglycerol formation in HEK293-DGAT1 cells (IC50=122 nM).
T863 causes weight loss, reduces serum and liver triglycerides, improves insulin sensitivity, and lowers serum cholesterol in diet-induced obese mice.
T863 is orally bioavailable.
