ChemicalBook CAS DataBase List 1441057-15-3

1441057-15-3

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
Molecular Formula	C24H21F6N5O2
Molecular Weight	525.45
MOL File	1441057-15-3.mol

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

Hazard Information

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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