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2477873-64-4

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2477873-64-4 Structure

2477873-64-4 Structure
IdentificationBack Directory
[Name]

BMS-986339
[CAS]

2477873-64-4
[Synonyms]

BMS-986339
Cyclobutanecarboxamide, N-[[4-[5-(1-fluoro-1-methylethyl)-1,2,4-oxadiazol-3-yl]bicyclo[2.2.2]oct-1-yl]methyl]-3-hydroxy-N-[4'-(1-hydroxy-1-methylethyl)[1,1'-biphenyl]-3-yl]-3-(trifluoromethyl)-, cis-
[Molecular Formula]

C35H41F4N3O4
[MOL File]

2477873-64-4.mol
[Molecular Weight]

643.71
Chemical PropertiesBack Directory
[Boiling point ]

724.7±70.0 °C(Predicted)
[density ]

1.321±0.06 g/cm3(Predicted)
[pka]

12.02±0.40(Predicted)
Hazard InformationBack Directory
[Uses]

BMS-986339 is an orally active, potent FXR agonist. BMS-986339 forms H-bond with His298 and ASN287 residues. BMS-986339 can be used in the research of primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), and nonalcoholic steatohepatitis (NASH), anti-fibrosis[1].
[in vivo]

BMS-986339 (compound 32, p.o., 10 mg/kg, once daily for 9 days) induces Fgf15 production, and shows antifibrotic efficacy in mouse bile duct ligation (BDL) model[1].
BMS-986339 (p.o. or i.v., 5 mg/kg or 1 mg/kg) exhibits low clearance and a long elimination half-life in mice and rats[1].

Animal Model:Mouse bile duct ligation (BDL) model[1]
Dosage:0.3, 1, 3, and 10 mg/kg, once daily for 9 days.
Administration:Oral administration
Result:Induced Fgf15 and SHP (small heterodimer partner) gene expression to a similar extent in the ileum.
Decreased the ratio of hydroxyproline to the total protein content, and decreased the collagen levels.
Animal Model:Male C57BL6 mice, male Sprague-Dawley rat (pharmacokinetic assay)[1]
Dosage:5 mg/kg or 1 mg/kg
Administration:Oral administration, intravenous injection
Result:Pharmacokinetic profile of BMS-986339 (compound 32).
parameter male C57BL6 mice male Sprague-Dawley rat
dose (mg/kg) i.v. 1 1
dose (mg/kg) p.o. 52
Vss (L/kg) i.v. 2.25.2
AUCtotal (μM?h) i.v. 16.46.6
AUCtotal (μM?h) p.o.56.65.8
t1/2 h (i.v.)1618
Fp.o.6940
[IC 50]

CYP2C8: 8 μM (IC50); CYP2C9: 13.5 μM (IC50)
[References]

[1] Susheel J Nara, et al. Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis. J Med Chem. 2022 Jul 14;65(13):8948-8960. DOI:10.1021/acs.jmedchem.2c00165
2477873-64-4 suppliers list
Company Name: ShangHai Caerulum Pharma Discovery Co., Ltd.  
Tel: 18149758185 18149758185;
Website: http://www.caerulumpharma.com
Company Name: Shanghai Jiegu Biotechnology Co., Ltd.  
Tel: 021-51698675
Website: www.jiejiegroup.com
Company Name: TargetMol Chemicals Inc.  
Tel: 15002134094
Website: https://www.targetmol.cn/
Company Name: Biorbyt Ltd.  
Tel: +44 (0)1223 859 353
Website: http://www.biorbyt.com
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