BMS 963272

MGAT-2抑制剂(IC50=7.1nM)；对MGAT-2具有选择性，优于MGAT-3、AWAT2和DGAT-2（所有药物的IC50=>33µM）；在高脂饮食诱发的肥胖症野生型而非Mogat2-/-小鼠模型中，以30mg/kg剂量降低体重增加和食物摄入量；在CDAHFD诱发的NASH小鼠模型中，以0.3和3mg/kg剂量降低血浆ALT、AST和胆汁酸水平以及肝纤维化。An MGAT-2 inhibitor (IC50 = 7.1 nM); selective for MGAT-2 over MGAT-3, AWAT2, and DGAT-2 (IC50s = >33 µM for all); reduces body weight gain and food intake in a wild-type but not Mogat2-/- mouse model of high-fat diet-induced obesity at 30 mg/kg; reduces plasma ALT, AST, and bile acid levels and hepatic fibrosis in a mouse model of CDAHFD-induced NASH at 0.3 and 3 mg/kg.分子式C24H21F6N5O2分子量525.4FC(F)([C@@]1(C2=CC=C(C=C2)OCCCC(F)(F)F)CC(C3=CC=C(C=C3)C)=C(C4=NN=NN4)C(N1)=O)F