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Obeticholic Acid(6-ECDCA INT-747)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Obeticholic Acid(6-ECDCA INT-747)图片
CAS NO:459789-99-2
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
Obeticholic Acid (INT747; 6-ECDCA; 6-Ethylchenodeoxycholic acid; trade name Ocaliva), a novel derivative of cholic acid, is a potent, orally bioactive and selective agonist of farnesoid X receptor (FXR) with EC50 of 99 nM, and has anticholeretic and anti-inflammatory activities. It is a semi-synthetic analog of bile acid which has the chemical structure 6α-ethyl-chenodeoxycholic acid. Obeticholic Acid was approved in 2016 for use as a drug to treat primary biliary cholangitis, and is undergoing development for several other liver diseases and related disorders. It displays anticholeretic activity in a rat model of cholestasis. It inhibits vascular smooth muscle cell inflammation and migration as well as promotes adipocyte differentiation and regulates adipose cell function in vivo.
理化性质和储存条件
Molecular Weight (MW)420.63
FormulaC26H44O4
CAS No.459789-99-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 84 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: 84 mg/mL (199.7 mM)
SMILES CodeC[C@@H]([C@H]1CC[C@@]2([H])[C@]3([H])[C@H](O)[C@H](CC)[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C)CCC(O)=O
SynonymsINT-747, 6-ECDCA; 6-Ethylchenodeoxycholic acid; Obeticholic acid; INT 747; INT747; Ocaliva.
实验参考方法
In Vitro

In vitro activity: Obeticholic Acid (also known as INT747; 6-ECDCA), a novel derivative of cholic acid, is a potent and selective agonist of farnesoid X receptor (FXR) with EC50 of 99 nM. It is a semi-synthetic analog of bile acid which has the chemical structure 6α-ethyl-chenodeoxycholic acid. Obeticholic Acid is used as a drug to treat primary biliary cholangitis, and is undergoing development for several other liver diseases and related disorders.


Kinase Assay: INT-747 is a potent and selective farnesoid X receptor (FXR) agonist with an EC50 of 99 nM.


Cell Assay: 6-ECDCA increases the expression of FXR-regulated genes in rat hepatocytes. INT-747 reduces expression of liver JNK-1 and JNK-2. INT-747 (256 μg/mL) shows complete inhibition of bacterial growth in all strains tested. Intestinal permeability remains unaffected after INT-747-addition to an IFN-γ-exposed intestinal epithelium of Caco-2 cells.

In VivoAdministration of LCA and its conjugates to rodents causes intrahepatic cholestasis,a pathogenic state characterized by decreased bile flow and the accumulation of bile constituents in the liver and blood. In DMH (dimethyldydrazine)-induced murine carcinogenesis model, LCA suppresses apoptosis almost completely in premalignant colon. LCA.
Animal modelRat cholestasis model
Formulation & DosageDissolved in saline; 7 μmol/kg/min; Infused at the right jugular vein using PE-50 polyethylene tubing
ReferencesJ Med Chem. 2002 Aug 15;45(17):3569-72; Am J Physiol Renal Physiol. 2009 Dec;297(6):F1587-96.