PF-06424439 methanesulfonate

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-06424439methylsulfonate 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 为 14 nM）。

PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor(IC50 of 14 nM). PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.(In Vivo):PF-06424439 methanesulfonate shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vdss) results in a short half-life.

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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 ratsDosage: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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Others

Other Targets

PI4Kα

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1469284-79-4

536.05

C23H30ClN7O4S

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (466.37 mM)

CS(O)(=O)=O.Clc1cnn(c1)C1(CC1)c1nc2ccc(nc2[nH]1)N1CCC[C@H](C1)C(=O)N1CCCC1

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(-20℃)

With Ice Pack

≥ 2 years