PF-05221304

ACC1和ACC2的抑制剂（IC50s分别为12.4和8.7nM）；抑制从头脂质合成（IC50=61nM）并增加原代人肝细胞中的脂肪酸氧化；减少原代人肝细胞中由从头衍生的脂肪酸组成的甘油三酯的积累；在10和100mg/kg剂量下减少大鼠肝脏丙二酰辅酶A的产生和从头脂肪生成；降低CDAHFD诱发的NASH大鼠模型中的肝纤维化、ALT和AST水平以及肝脏甘油三酯的积累。An inhibitor of ACC1 and ACC2 (IC50s = 12.4 and 8.7 nM, respectively); inhibits de novo lipid synthesis (IC50 = 61 nM) and increases fatty acid oxidation in primary human hepatocytes; reduces the accumulation of triglycerides composed of de novo-derived fatty acids in primary human hepatocytes; reduces hepatic malonyl-CoA production and de novo lipogenesis in rats at 10 and 100 mg/kg; reduces hepatic fibrosis, ALT and AST levels, and hepatic triglyceride accumulation in a rat model of CDAHFD-induced NASH.分子式C28H30N4O5分子量502.6O=C(C1=CC=C(C2=CC(C(N3CCC4(CC3)CC(C5=C(C4)C=NN5C(C)C)=O)=O)=CC(OC)=N2)C=C1)O