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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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货号: HY-108339
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