2. Metabolic Enzyme/Protease
  3. FXR Cytochrome P450
  4. BMS-986339

BMS-986339 是一种具有口服活性的 FXR 激动剂。BMS-986339 可与 His298 和 ASN287 残基形成氢键。BMS-986339 可用于原发性胆汁性肝硬化 (PBC)、原发性硬化性胆管炎 (PSC)、非酒精性脂肪性肝炎 (NASH)，和抗纤维化研究。

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BMS-986339 Chemical Structure

BMS-986339 Chemical Structure

CAS No. : 2477873-64-4

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BMS-986339 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target[1]

CYP2C8

8 μM (IC50)

CYP2C9

13.5 μM (IC50)

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

BMS-986339 相关抗体:
体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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. 5 2
Vss (L/kg) i.v. 2.2 5.2
AUCtotal (μM•h) i.v. 16.4 6.6
AUCtotal (μM•h) p.o. 56.6 5.8
t1/2 h (i.v.) 16 18
Fp.o. 69 40
分子量

643.71

Formula

C35H41F4N3O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BMS-986339 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-9863392477873-64-4BMS986339BMS 986339FXRCytochrome P450NR1H4CYPsNASHanti-fibrosisbile acidPBCPSCfibrosisBDL modelBSEPInhibitorinhibitorinhibit

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