产品
编 号：F753120
分子式：C35H41F4N3O4
分子量：643.71
分子式：C35H41F4N3O4
分子量：643.71
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CAS No: 2477873-64-4
产品详情
生物活性：
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.
体内研究：
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.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.Animal Model:Mouse bile duct ligation (BDL) model
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)
Dosage:5 mg/kg or 1 mg/kg
Administration:Oral administration, intravenous injection
Result:Pharmacokinetic profile of BMS-986339 (compound 32).parameter male C57BL6 micemale 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
体外研究：
BMS-986339 (compound 32, 0.1 nM-10 μM, 24 h) reduces activation of genes expressing BSEP (bile salt export pump) in Huh-7 cells, and FGF19 in hepatocytes.BMS-986339 inhibits cytochrome P450 activity (IC50: 8 μM (CYP2C8), 13.5 μM (CYP2C9)), and inhibits hERG channel in a patch clamp assay(IC50: 4.5 μM).BMS-986339 inhibits transporters OATP1B3 and BSEP with IC50 values of 1.44 and 1.5 μM, and hUGT1A1 (IC50: 4.85 μM).
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.
体内研究：
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.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.Animal Model:Mouse bile duct ligation (BDL) model
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)
Dosage:5 mg/kg or 1 mg/kg
Administration:Oral administration, intravenous injection
Result:Pharmacokinetic profile of BMS-986339 (compound 32).parameter male C57BL6 micemale 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
体外研究：
BMS-986339 (compound 32, 0.1 nM-10 μM, 24 h) reduces activation of genes expressing BSEP (bile salt export pump) in Huh-7 cells, and FGF19 in hepatocytes.BMS-986339 inhibits cytochrome P450 activity (IC50: 8 μM (CYP2C8), 13.5 μM (CYP2C9)), and inhibits hERG channel in a patch clamp assay(IC50: 4.5 μM).BMS-986339 inhibits transporters OATP1B3 and BSEP with IC50 values of 1.44 and 1.5 μM, and hUGT1A1 (IC50: 4.85 μM).
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