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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。
PF-06424439图片
CAS NO:1469284-78-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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 t1/2=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.