PF-06424439

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PF-06424439

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1469284-78-3

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

生物活性

PF-06424439 is an oral, potent and selective imidazopyridinediacylglycerolacyltransferase2 (DGAT2)inhibitor with anIC₅₀of 14 nM^[1]. PF-06424439 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]

体内研究
(In Vivo)

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^-/-)^[1].
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^[1].

Animal Model:	Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr^-/-)^[1]
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^[1]
Dosage:	1 mg/kg
Administration:	I.v.
Result:	Showed moderate clearance and a short half-life with t_1/2=1.39 h.

分子量

439.94

Formula

C₂₂H₂₆ClN₇O

CAS 号

1469284-78-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.