Catalog No.S7660 Synonyms: INT-747, 6-ECDCA
Molecular Weight(MW): 420.63
Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Phase 3.
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(D) Expression of hepatic FXR target genes, n = 3. Data are expressed as mean ± SD, ###P < 0.001 versus group 1, *P < 0.05, **P < 0.01, and ***P b 0.001 versus group 2, sP < 0.05, ssP < 0.01, and sssP < 0.001 versus group 3
Toxicol Appl Pharmacol, 2017, 315:23-34. Obeticholic Acid purchased from Selleck.
(c) Functional bile canaliculi or lack thereof in PHHs within MPTCs (12 d of drug treatment) as visualized by transport of fluorescent (green) dye into the canaliculi between PHHs. DMSO-treated MPCC control image is shown to the far right. (d) Neutral lipid (Nile red, green) staining of PHHs within MPTCs (12 d of drug treatment). DMSO-treated MPCC control image is shown to the far right. (e) NR1I2 (PXR) gene expression in drug-treated MPTCs relative to DMSOtreated MPTC controls (12 d of treatment). (f) ABCC2 (MRP2) gene expression in drug-treated MPTCs relative to DMSO-treated MPTC controls (12 d of treatment). (g) IL-6 levels in drug-treated MPTC supernatants (6 d of treatment). In all panels, statistical significance is displayed relative to DMSO-treated MPTCs. *p r 0.05, **p r 0.01, ***p r 0.001, and ****p r 0.0001. Scale bars on images represent 80 mm.
Integr Biol (Camb), 2017, 9(8):662-677. Obeticholic Acid purchased from Selleck.
Purity & Quality Control
Choose Selective FXR Inhibitors
|Description||Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Phase 3.|
In HuH7 cells, Obeticholic Acid acts as a potent FXR agonist with EC50 of 85 nM. 
|In vivo||In rat cholestasis model, Obeticholic Acid promotes bile flow, and protects hepatocytes against acute necrosis caused by LCA.  Obeticholic Acid (p.o.) improves proteinuria, ameliorates renal structural changes, and modulates renal inflammation and oxidative stress in WD-fed DBA mice.  In thioacetamide (TAA)-intoxicated and bile-duct-ligated (BDL) rats, Obeticholic Acid (30 mg/kg p.o.) reactivates the FXR downstream signaling pathway and decreases portal pressure by lowering total IHVR without deleterious systemic hypotension. |
|In vitro||DMSO||84 mg/mL (199.7 mM)|
|Ethanol||84 mg/mL warmed (199.7 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02177136||Completed||Primary Sclerosing Cholangitis (PSC)||Intercept Pharmaceuticals||February 9 2015||Phase 2|
|NCT02633956||Completed||Nonalcoholic Steatohepatitis||Intercept Pharmaceuticals||December 4 2015||Phase 2|
|NCT03439254||Recruiting||Compensated Cirrhosis|Nonalcoholic Steatohepatitis||Intercept Pharmaceuticals||August 30 2017||Phase 3|
|NCT02430077||Recruiting||Familial Partial Lipodystrophy||University of Texas Southwestern Medical Center||June 2016||Phase 2|
|NCT02548351||Recruiting||Non Alcoholic Steatohepatitis (NASH)||Intercept Pharmaceuticals||September 2015||Phase 3|
|NCT02532335||Recruiting||Obesity||Sahlgrenska University Hospital Sweden||August 2015||Phase 1|
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Frequently Asked Questions
What formulation can we use to dissolve Obeticholic Acid (Catalog No.S7660) for mice in vivo study?
You can use the vehicle of: 1% wt/vol methyl-cellulose as indicated in this paper, http://www.sciencedirect.com/science/article/pii/S0925443911000883 "daily oral gavage with 5 mg/kg/day INT-747 (6-ethyl-chenodeoxycholic acid, Obeticholic acid, Intercept Pharmaceuticals Inc, New York, NY) or vehicle (1% wt/vol methyl-cellulose) from 3 days prior to induction of colitis"