product name Obeticholic Acid
Description: Obeticholic Acid (also known as INT747; 6-ECDCA) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. It is a novel derivative of cholic acid which 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.
References: J Med Chem. 2002 Aug 15;45(17):3569-72; Am J Physiol Renal Physiol. 2009 Dec;297(6):F1587-96.
420.63
Formula
C26H44O4
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)
Solubility (In vivo)
Synonyms
INT-747, 6-ECDCA
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19421707
| In Vitro |
In vitro activity: In HuH7 cells, Obeticholic Acid acts as a potent FXR agonist with EC50 of 85 nM. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Administration 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 model | Rat cholestasis model |
| Formulation & Dosage | Dissolved in saline; 7 μmol/kg/min; Infused at the right jugular vein using PE-50 polyethylene tubing |
| References | J Med Chem. 2002 Aug 15;45(17):3569-72; Am J Physiol Renal Physiol. 2009 Dec;297(6):F1587-96. |
