DGAT1-IN-4 is a potent, selective, and orally efficacious inhibitor of DGAT-1 with IC50 of 15 nM and 9 nM for hDGAT-1 and mDGAT-1, respectively.
DGAT1-IN-4 shows no significant activity for ACAT-1 (IC50=5.2 uM).
DGAT1-IN-4 shows effectivity in both intestinal and adipose tissue, reduces body weight or body weight gain following oral administration in both mouse and rat models of dietary-induced obesity.
