| Bioactivity | 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]. |
| Invitro | 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[1].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)[1].BMS-986339 inhibits transporters OATP1B3 and BSEP with IC50 values of 1.44 and 1.5 μM, and hUGT1A1 (IC50: 4.85 μM)[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: |
| Name | BMS-986339 |
| CAS | 2477873-64-4 |
| Formula | C35H41F4N3O4 |
| Molar Mass | 643.71 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
BMS-986339
CAS: 2477873-64-4 F: C35H41F4N3O4 W: 643.71
BMS-986339 is an orally active, potent FXR agonist. BMS-986339 forms H-bond with His298 and ASN287 residues. BMS-986339
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.