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| | 2(1H)-Pyridinone, 5,6-dihydro-4-(4-methylphenyl)-3-(2H-tetrazol-5-yl)-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-, (6S)- Basic information |
| Product 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)- | | Synonyms: | 2(1H)-Pyridinone, 5,6-dihydro-4-(4-methylphenyl)-3-(2H-tetrazol-5-yl)-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-, (6S)-;BMS-963272 | | CAS: | 1441057-15-3 | | MF: | C24H21F6N5O2 | | MW: | 525.45 | | EINECS: | | | Product Categories: | | | Mol File: | 1441057-15-3.mol | ![2(1H)-Pyridinone, 5,6-dihydro-4-(4-methylphenyl)-3-(2H-tetrazol-5-yl)-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-, (6S)- Structure](CAS/20210305/GIF/1441057-15-3.gif) |
| | 2(1H)-Pyridinone, 5,6-dihydro-4-(4-methylphenyl)-3-(2H-tetrazol-5-yl)-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-, (6S)- Chemical Properties |
| 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 |
| | 2(1H)-Pyridinone, 5,6-dihydro-4-(4-methylphenyl)-3-(2H-tetrazol-5-yl)-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-, (6S)- Usage And Synthesis |
| 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. |
| | 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. |
| | 2(1H)-Pyridinone, 5,6-dihydro-4-(4-methylphenyl)-3-(2H-tetrazol-5-yl)-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-, (6S)- Preparation Products And Raw materials |
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