Obeticholic Acid Obeticholic Acid (INT-747, 6-ECDCA, 6-Ethylchenodeoxycholic acid) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy . Phase 3. In vitro
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. Cell Data