PF-04620110 is a potent, selective, orally bioavailable DGAT-1 inhibitor with IC50 of 19 nM, shows no acitivity for DGAT-2 (IC50>30 uM).
PF-04620110 shows high selectivity versus a broad panel of off-target pharmacologic end points.
PF-04620110 inhibits triglyceride synthesis of 3 in the intestinal-derived HT-29 cell line with IC50 of 8 nM.
PF-04620110 demonstrates in vivo DGAT-1 inhibitionthrough reduction of plasma triglyceride levels in rodent, alters the temporal and spatial pattern of dietary lipid absorption in vivo.
