INT-747

SKU: orb1225018

Description

INT-747(Obeticholic acid, 6-ECDCA, 6-Ethylchenodeoxycholic acid) is a potent and selective FXR agonist (EC50=99 nM); possesses anticholeretic activity in rat model of cholestasis.Other Indication Approved.

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 459789-99-2
• MW: 420.6252
• Purity: >98% (HPLC)
• Formula: C₂₆H₄₄O₄
• SMILES: C[C@@H]([C@H]1CC[C@@]2([H])[C@]3([H])[C@H](O)[C@H](CC)[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C)CCC(O)=O
• Target: FXR
• Solubility: DMSO: ≥ 33 mg/mL

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Obeticholic acid | 6-ECDCA | 6-Ethylchenodeoxycholic acid

Quick Database Links

Gene Symbol

FXR