| Identification | Back Directory | [Name]
2(1H)-Pyridinone, 5,6-dihydro-4-(4-methylphenyl)-3-(2H-tetrazol-5-yl)-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-, (6S)- | [CAS]
1441057-15-3 | [Synonyms]
BMS-963272
2(1H)-Pyridinone, 5,6-dihydro-4-(4-methylphenyl)-3-(2H-tetrazol-5-yl)-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-, (6S)- | [Molecular Formula]
C24H21F6N5O2 | [MOL File]
1441057-15-3.mol | [Molecular Weight]
525.45 |
| Chemical Properties | Back Directory | [density ]
1.395±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 250 mg/mL (475.78 mM; Need ultrasonic) | [form ]
Solid | [pka]
4.04±0.10(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
BMS-963272 is an orally active and selective MGAT2 inhibitor (IC50 = 7.1 nM), used for the study of metabolic disorders and inflammatory diseases[1][2]. | [Biological Activity]
BMS-963272 is a potent, selective MGAT2 inhibitor (IC50 = 7.1 nM) for the treatment of metabolic disorders. | [in vivo]
BMS-963272 (30 mg/kg, p.o., twice daily, for 24 days) reduced body weight gain and significantly decreased food intake in the diet-induced obese mouse model[1].
BMS-963272 (0.3 and 3.0 mg/kg, p.o., once daily, for 8 weeks) exhibited potent antifibrotic and anti-inflammatory effects in the choline-deficient, amino acid-defined high-fat diet (CDAHFD)-induced non-alcoholic steatohepatitis (NASH) mouse model by reducing liver fibrosis and lowering the expression of inflammatory markers such as tumor necrosis factor-alpha (TNFa), further improving liver function as evidenced by decreased alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels[2]. | Animal Model: | Diet-induced obese mouse model (C57BL/6J)[1] | | Dosage: | 30 mg/kg | | Administration: | Oral gavage (p.o.), twice daily, for 24 days | | Result: | Reduced body weight gain by 8.6%-14.3%; significantly decreased food intake by 18%-27%. |
| Animal Model: | CDAHFD-induced NASH mouse (C57BL/6J mice) model (CDAHFD: Choline-Deficient, Amino Acid-Defined High Fat Diet)[2] | | Dosage: | 0.3 mg/kg and 3.0 mg/kg | | Administration: | Oral gavage (p.o.), once daily, for 8 weeks | | Result: | Significantly reduced liver fibrosis, decreased ALT and AST levels, and reduced TNFa expression. |
| [storage]
Store at -20°C | [References]
[1]. Turdi H, et al. Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders. J Med Chem. 2021 Oct 14;64(19):14773-14792. |
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