Obeticholic Acid (INT747; 6-ECDCA) is a novel derivative of cholic acid which acts as a potent and selective FXR agonist displaying anticholeretic activity in an in vivo 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.
CAS Number: 459789-99-2
Molecular Weight: 420.63
Chemical Name: (4R)-4-[(3R,5S,6R,7R,8S,9S,10S,13R,14S,17R)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
Obeticholic acid (INT-747) increases the expression of FXR-regulated genes in rat hepatocytes. Obeticholic acid (INT-747) reduces expression of liver JNK-1 and JNK-2. Obeticholic acid (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.
Obeticholic acid (INT-747) (10 mg/kg/day) completely reverted cholestasis induced by E217α. Administration of Obeticholic acid (INT-747) partially prevents the impairment in total bile acid output caused by E217α by increasing the relative abundance of β-MCA and TCDCA and TDCA. Obeticholic acid (INT-747)7 (10 mg/kg) and HS increases the pulmonary congestion in the animals. INT-747 does not improve renal pathology in the HS-fed animals. Obeticholic acid (INT-747) (5 mg/kg) significantly increases survival in BDL rats. Obeticholic acid (INT-747)-treated BDL rats exhibits a significant selective ileal increase in expression of pore-closing claudin-1. Ileal expression of ZO-1 is significantly up-regulated in INT-747-treated BDL rats.
- LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases;
- Fiorucci S, Di Giorgio C, Distrutti E. Obeticholic Acid: An Update of Its Pharmacological Activities in Liver Disorders. Handb Exp Pharmacol. 2019;256:283-295. doi: 10.1007/164_2019_227. Review. PubMed PMID: 31201552.
- Patient Group Input Submissions: Obeticholic Acid (Ocaliva): (Intercept Pharma Canada, Inc.): Indication: For the treatment of primary biliary cholangitis [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health;
- Pharmacoeconomic Review Report: Obeticholic Acid (Ocaliva): (Intercept Pharma Canada, Inc.): Indication: For the treatment of primary biliary cholangitis [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health;
- CADTH Canadian Drug Expert Committee Recommendation: Obeticholic Acid (Ocaliva — Intercept Pharmaceuticals Canada): Indication: Primary biliary cholangitis [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health;
Products are for research use only. Not for human use.
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