PF-06471553

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。

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库存: 现货

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促销价

数量
5mg

￥5175.00

4140.00

- +
10mg

￥7987.00

6390.00

- +
25mg

￥14962.00

11970.00

- +
50mg

￥25637.00

20510.00

- +
100mg

￥36825.00

29460.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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Background

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.