An MGAT-2 inhibitor
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BMS 963272

Item No. 34981

Technical Information
Formal Name
(6S)-5,6-dihydro-4-(4-methylphenyl)-3-(2H-tetrazol-5-yl)-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-2(1H)-pyridinone
CAS Number
1441057-15-3
Molecular Formula
C24H21F6N5O2
Formula Weight
Purity
≥98%
Formulation
A solid
SMILES
FC(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
InChi Code
InChI=1S/C24H21F6N5O2/c1-14-3-5-15(6-4-14)18-13-22(24(28,29)30,31-21(36)19(18)20-32-34-35-33-20)16-7-9-17(10-8-16)37-12-2-11-23(25,26)27/h3-10H,2,11-13H2,1H3,(H,31,36)(H,32,33,34,35)/t22-/m0/s1
InChi Key
AEMPUAWUDAMJBV-QFIPXVFZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BMS 963272 is an inhibitor of monoacylglycerol acyltransferase 2 (MGAT-2; IC50 = 7.1 nM).1 It is selective for MGAT-2 over MGAT-3, acyl-CoA wax alcohol acyltransferase 2 (AWAT2), and diacylglycerol acyltransferase 2 (DGAT-2; IC50s = >33 µM for all). In vivo, BMS 963272 (30 mg/kg) reduces body weight gain and food intake in a wild-type but not Mogat2-/- mouse model of high-fat diet-induced obesity. BMS 963272 (0.3 and 3 mg/kg) reduces plasma alanine transaminase (ALT), aspartate aminotransferase (AST), and bile acid levels and hepatic fibrosis in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a choline-deficient and high-fat diet (CDAHFD).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Turdi, H., Chao, H., Hangeland, J.J., et alScreening hit to clinical candidate: Discovery of BMS-963272, a potent, selective MGAT2 inhibitor for the treatment of metabolic disorders. J. Med. Chem. 64(19), 14773-14792 (2021).

    2. Cheng, D., Zinker, B.A., Luo, Y., et alMGAT2 inhibitor decreases liver fibrosis and inflammation in murine NASH models and reduces body weight in human adults with obesity. Cell Metab. 34(11), 1732-1748 (2022).