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PF-06471553
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-06471553图片
CAS NO:1808094-07-6
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)询价
5mg询价
10mg询价
25mg询价
50mg询价
100mg询价

PF-06471553是一种有效的,选择性的,可口服的monoacylglycerolacyltransferase3(MGAT3)抑制剂,IC50值为92nM。
Cas No.1808094-07-6
Canonical SMILESO=S(C1=CC2=C(CN(C(CC3=CC=CC(OC)=C3)=O)C2)C=C1)(NC4=NN(C5CCC5)N=C4)=O
分子式C23H25N5O4S
分子量467.54
溶解度DMSO : ≥ 150 mg/mL (320.83 mM)
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-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.

PF-06471553 (6f) is a potent and selective monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM, and shows >160 fold in vitro selectivity for MGAT3 over DGAT1 (IC50, >50 μM), DGAT2 (IC50, >100 μM), MGAT1 (IC50, 14.9 μM), and MGAT2 (IC50, 19.8 μM). PF-06471553 exhibits inhibitory activity against MGAT3 in HEK-293 cells with an IC50 of 205 nM (pIC50, 6.69)[1].

PF-06471553 (200 mg/kg, p.o.) in addition with (DGAT1 and DGAT2) inhibitors shows additional inhibition of glycerol-d5 incorporated triolein in hMGAT3 mice, and with no effect on WT mice[1].

[1]. Huard K, et al. Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3. J Med Chem. 2015 Sep 24;58(18):7164-72.

 
 
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