PF-06424439 methanesulfonate 是一种口服有效咪唑并吡啶二酰基甘油酰基转移酶 2 (DGAT2)选择性抑制剂，IC50是14 nM。PF-06424439 methanesulfonate具有缓慢可逆，时间依赖性的特点，其相对于酰基-CoA 底物以非竞争性模式抑制 DGAT2。

PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor(IC50 of 14 nM)[1]. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate[2].

PF-06424439 methanesulfonate shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vdss) results in a short half-life[1].

PF-06424439 methanesulfonate (i.v.; 1 mg/kg) shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vdss) results in a short half-life[1].PF-06424439 methanesulfonate (p.o.; 60 mg/kg/day; for 3 days) reduces plasma TG and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-)[1].

1469284-79-4

C23H30ClN7O4S

536.05

H2O:99 mg/mL (184.68 mM)
DMSO:249 mg/mL (464.50 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years