PF-06424439 (methanesulfonate)

1469284-79-4

536.05

DMSO : 250 mg/mL (466.37 mM; Need ultrasonic)

Metabolic Enzyme/Protease

PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an 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]. IC50 & Target: IC50: 14 nM (DGAT2)^[1] In Vivo: 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].
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].