产品
编 号：F170734
分子式：C22H26ClN7O
分子量：439.94
分子式：C22H26ClN7O
分子量：439.94
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CAS No: 1469284-78-3
产品详情
生物活性：
PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
体内研究：
PF-06424439 (p.o.; 60 mg/kg/day; for 3 days) reduces plasma triglyceride (TG) and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-).PF-06424439 (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.Animal Model:Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr-/-)
Dosage:60 mg/kg
Administration:P.o.; daily; for 3 days
Result:Reduced plasma TG and cholesterol levels and decreased nonsignificant in circulating lipids.
Animal Model:Male Wistar-Han rats
Dosage:1 mg/kg
Administration:I.v.
Result:Showed moderate clearance and a short half-life with t1/2=1.39 h.
PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
体内研究：
PF-06424439 (p.o.; 60 mg/kg/day; for 3 days) reduces plasma triglyceride (TG) and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-).PF-06424439 (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.Animal Model:Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr-/-)
Dosage:60 mg/kg
Administration:P.o.; daily; for 3 days
Result:Reduced plasma TG and cholesterol levels and decreased nonsignificant in circulating lipids.
Animal Model:Male Wistar-Han rats
Dosage:1 mg/kg
Administration:I.v.
Result:Showed moderate clearance and a short half-life with t1/2=1.39 h.
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