1. Metabolic Enzyme/Protease
  2. FXR

INT-747 (Synonyms: Obeticholic acid; 6-ECDCA; 6-Ethylchenodeoxycholic acid)

Cat. No.: HY-12222 Purity: >98.0%
Data Sheet SDS Handling Instructions

INT-747 is a potent and selective FXR agonist (EC50=99 nM) endowed with anticholestatic activity.

For research use only. We do not sell to patients.
INT-747 Chemical Structure

INT-747 Chemical Structure

CAS No. : 459789-99-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
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10 mg $70 In-stock
50 mg $240 In-stock
100 mg $350 In-stock
200 mg $550 In-stock
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  • References

Description

INT-747 is a potent and selective FXR agonist (EC50=99 nM) endowed with anticholestatic activity.

IC50 & Target

EC50: 99 nM (FXR)

In Vitro

6-ECDCA increases the expression of FXR-regulated genes in rat hepatocytes[1]. INT-747 reduces expression of liver JNK-1 and JNK-2[2]. 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[3].

In Vivo

6-ECDCA (10 mg/kg/day) completely reverted cholestasis induced by E217α. Administration of 6-ECDCA partially prevents the impairment in total bile acid output caused by E217α by increasing the relative abundance of β-MCA and TCDCA and TDCA[1]. INT-747 (10 mg/kg) and HS increases the pulmonary congestion in the animals.INT-747 does not improve renal pathology in the HS-fed animals[2]. INT-747 (5 mg/kg) significantly increases survival in BDL rats. 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[3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00501592 Intercept Pharmaceuticals Diabetes Mellitus, Type II|Fatty Liver July 2007 Phase 2
NCT00550862 Intercept Pharmaceuticals Liver Cirrhosis, Biliary October 2007 Phase 2
NCT00570765 Intercept Pharmaceuticals Liver Cirrhosis, Biliary November 2007 Phase 2
NCT01585025 Imperial College London Primary Bile Acid Malabsorption|Secondary Bile Acid Malabsorption|Chronic Diarrhoea April 2012 Phase 2
NCT02430077 University of Texas Southwestern Medical Center Familial Partial Lipodystrophy June 2016 Phase 2
NCT01265498 National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) Nonalcoholic Fatty Liver Disease (NAFLD)|Nonalcoholic Steatohepatitis (NASH) March 2011 Phase 2
NCT02039219 Naga P. Chalasani|National Institute on Alcohol Abuse and Alcoholism (NIAAA)|Intercept Pharmaceuticals|Indiana University Alcoholic Hepatitis November 2014 Phase 2
NCT02548351 Intercept Pharmaceuticals Non Alcoholic Steatohepatitis (NASH) September 2015 Phase 3
NCT01625026 Sahlgrenska University Hospital, Sweden|Medical University of Vienna Obesity|Gallstones September 2013 Phase 2
NCT02308111 Intercept Pharmaceuticals Liver Cirrhosis, Biliary December 2014 Phase 4
NCT02532335 Sahlgrenska University Hospital, Sweden Obesity August 2015 Phase 1
NCT01865812 Intercept Pharmaceuticals Primary Biliary Cirrhosis November 2013 Phase 2
NCT01904539 Intercept Pharmaceuticals Hepatic Impairment June 2013 Phase 1
NCT01473524 Intercept Pharmaceuticals Primary Biliary Cirrhosis January 2012 Phase 3
NCT02633956 Intercept Pharmaceuticals Nonalcoholic Steatohepatitis December 2015 Phase 2
NCT02654236 Suthat Liangpunsakul|National Institute on Alcohol Abuse and Alcoholism (NIAAA)|Intercept Pharmaceuticals|Indiana University Alcohol Consumption April 2016
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.3774 mL 11.8869 mL 23.7739 mL
5 mM 0.4755 mL 2.3774 mL 4.7548 mL
10 mM 0.2377 mL 1.1887 mL 2.3774 mL
Animal Administration
[2]

INT-747 is formulated in 1% methylcellulose in distilled water.

Initially, all animals (at 6-weeks age) are placed on a standard rodent diet for a week. Baseline blood and urine samples are collected and basal blood pressure (BP) is measured prior to grouping the animals. Subsequently, the animals are randomized into low (LS; n=9) or high salt (HS) diet groups. Hypertension is induced in the HS group by daily high-salt diet feeding and the group is subdivided to receive one of two doses of INT-747: low dose (10 mg/kg/day; n=15) or high dose (30 mg/kg/day; n=15) in 1% methylcellulose; or vehicle (1% methylcellulose in distilled water; n=15) orally everyday for 6 weeks. In parallel, the LS group also receive 1% methylcellulose. BP is measured weekly for the duration of the study as described below. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

420.63

Formula

C₂₆H₄₄O₄

CAS No.

459789-99-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 33 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: >98.0%

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INT-747
Cat. No.:
HY-12222
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