PF-06424439

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-06424439 是一种口服选择性咪唑吡啶二酰基甘油酰基转移酶 2 (DGAT2) 抑制剂（IC50 为 14 nM）。

PF-06424439 is an oral and selective inhibitor of imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) (IC50 of 14 nM).

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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 daysResult: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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Metabolic Enzyme/Protease

Transferase

DGAT2

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1469284-78-3

439.94

C22H26ClN7O

>98% (HPLC)

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O=C([C@H](CCC1)CN1c(cc1)nc2c1nc(C1(CC1)n1ncc(Cl)c1)[nH]2)N1CCCC1

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(-20℃)

With Ice Pack

≥ 2 years