PF-06471553,1808094-07-6

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PF-06471553

CAS No. : 1808094-07-6

MCE 国际站：PF-06471553

产品活性：PF-06471553 是一种有效的，选择性的，可口服的 monoacylglycerol acyltransferase 3 (MGAT3) 抑制剂，IC₅₀ 值为 92 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Acyltransferase

In Vitro: 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).

In Vivo: 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.

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