Obeticholic Acid

SKU: orb1307446

Description

Obeticholic Acid (6-ECDCA, INT-747) is a potent semisynthetic FXR agonist (EC50 = 99 nM) that induces IκB-α, KLF-2, and KLF-4 expression. It is widely used in research on metabolic and liver diseases, including studies in vitro and in vivo for hepatic steatosis, fibrosis, inflammation, and insulin resistance.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 459789-99-2
• MW: 420.63
• Purity: 99.97% (May vary between batches)
• Formula: C₂₆H₄₄O₄
• SMILES: CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@H]([C@H](C)CCC(O)=O)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12
• Target: Autophagy,FXR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.89 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:237.5 mg/mL (564.63 mM);Ethanol:78 mg/mL (185.44 mM)

Bioactivity

• Target IC50:
  FXR:99 nM(EC50)
• In Vivo:
  METHODS: Thioacetamide (TAA)-intoxicated and bile duct ligation (BDL) rats were used as models. Two oral doses of 30 mg/kg obeticholic acid (INT-747) were administered within 24 hours to evaluate in vivo hemodynamics. The effects of short-term obeticholic acid (INT-747) treatment on intrahepatic hemodynamic dysfunction and signaling pathways in different rat models of cirrhotic portal hypertension (PHT) were investigated. RESULTS FXR expression was decreased in both cirrhotic models. Obeticholic acid (INT-747) administration in TAA and BDL reactivated FXR downstream signaling pathways and reduced portal pressure by reducing total IHVR without causing harmful systemic hypotension. Obeticholic acid (INT-747) improved endothelial vasodilation but not hyperresponsiveness in perfused TAA and BDL cirrhotics. METHODS: Animals were fed a low-salt (control) or high-salt diet and treated with obeticholic acid (6-ECDCA, INT-747) (10, 30 mg/kg/day, oral, 6 weeks). Liver lysates were compared for c-JNK1 and 2 expression by Western blot. RESULTS INT-747 reduced hepatic JNK-1 and JNK-2 expression; proinflammatory proteins may be upregulated by a high-salt diet, thereby interfering with normal insulin signaling.
• In Vitro:
  METHODS: SCC cells were treated with increasing concentrations of obeticholic acid (6-ECDCA, INT-747) (0-100 μM), hepatocytes and HSCs were seeded at the same density and treated with obeticholic acid (6-ECDCA, INT-747) (0.1, 1 and 10 μM), and finally MTT assay was performed. RESULTS Obeticholic acid (6-ECDCA, INT-747) reduced cell viability by more than 20% at a concentration of 10 μM.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Obeticholic Acid, orally, NR1H4, inhibit, INT 747, INT747, INT-747, Inhibitor, FXR, farnesoid, 6-ECDCA, 6-Ethylchenodeoxycholic acid, active, Autophagy, receptor

Compound Identifiers

PubChem CID

447715