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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:1469284-79-4
包装与价格：
包装价格(元)
10mM 1 mL in DMSO电议
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
PF-06424439 是一种口服的、有效的、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。
Cas No.1469284-79-4
化学名[(3R)-1-[2-[1-(4-chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone, monomethanesulfonate
Canonical SMILESO=C(N1CCCC1)[C@@H]2CCCN(C3=NC(N=C(C4(CC4)N5N=CC(Cl)=C5)N6)=C6C=C3)C2.OS(C)(=O)=O
分子式C22H26ClN7O.CH3SO3H
分子量536
溶解度DMSO: soluble,Water: soluble
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM[1]. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate[2].

PF-06424439 methanesulfonate (p.o.; 60 mg/kg/day; for 3 days) reduces plasma TG and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-)[1].PF-06424439 methanesulfonate (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].

References:
[1]. Futatsugi K, et al. Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). J Med Chem. 2015 Sep 24;58(18):7173-85.
[2]. Pabst B, et al. Mechanistic Characterization of Long Residence Time Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). Biochemistry. 2018 Dec 26;57(51):6997-7010.