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Obeticholic Acid

Catalog No.
B4888
FXR agonist with anticholeretic activity
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$61.00
In stock
5mg
$55.00
In stock
25mg
$165.00
In stock
100mg
$220.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Obeticholic Acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECDCA, INT-747) is a potent and selective agonist of FXR with EC50 value of 99 nM [1].

The farnesoid X receptor (FXR) is a nuclear bile acid receptor involved in bile acid homeostasis, liver fibrosis, hepatic and intestinal inflammation and cardiovascular disease [2].

Obeticholic Acid is a potent and selective FXR agonist with anticholeretic activity [1]. Obeticholic Acid is a semisynthetic bile acid derivative and potent FXR ligand. In estrogen-induced cholestasis rats, 6-ECDCA protected against cholestasis induced by 17α-ethynylestradiol (E217α) [2]. In cirrhotic portal hypertension (PHT) rat models, INT-747 (30 mg/kg) reactivated the FXR downstream signaling pathway and reduced portal pressure by lowering total intrahepatic vascular resistance (IHVR) without deleterious systemic hypotension. This effect was associated with an increased eNOS activity [3]. In the Dahl rat model of salt-sensitive hypertension and insulin-resistance (IR), high salt (HS) diet significantly increased systemic blood pressure and downregulated tissue DDAH expression. INT-747 enhanced insulin sensitivity and inhibited the decrease of DDAH expression [4].

References:
[1].? Pellicciari R, Fiorucci S, Camaioni E, et al. 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. J Med Chem, 2002, 45(17): 3569-3572.
[2].? Fiorucci S,?Clerici C,?Antonelli E,?et al. Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis. J Pharmacol Exp Ther, 2005, 313(2): 604-612.
[3].? Verbeke L, Farre R, Trebicka J, et al. Obeticholic acid, a farnesoid X receptor agonist, improves portal hypertension by two distinct pathways in cirrhotic rats. Hepatology, 2014, 59(6): 2286-2298.
[4].? Ghebremariam YT, Yamada K, Lee JC, et al. FXR agonist INT-747 upregulates DDAH expression and enhances insulin sensitivity in high-salt fed Dahl rats. PLoS One, 2013, 8(4): e60653.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt420.63
Cas No.459789-99-2
FormulaC26H44O4
Solubility≥21.5 mg/mL in DMSO; insoluble in H2O; ≥21.3 mg/mL in EtOH
Chemical Name(4R)-4-[(3R,5S,6R,7R,8S,9S,10S,13R,14S,17R)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid
SDFDownload SDF
Canonical SMILESCCC1C2CC(CCC2(C3CCC4(C(C3C1O)CCC4C(C)CCC(=O)O)C)C)O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

Rat hepatocytes

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

24 h

Applications

In rat hepatocytes, obeticholic acid transactivates FXR and modulates FXR regulated genes, resulting in increases of Shp and bsep mRNA expression by 3 to 5 fold and reduction of cyp7a1, cyp8b1, and ntcp mRNA expression by 50 to 70% after exposure to FXR ligands.
Animal experiment [2]:

Animal models

Male Wistar rats weighing 200-250 g

Dosage form

30 mg/kg

Preparation method

Dissolved in 0.75-1.0 mL of freshly prepared methylcellulose (1%)

Applications

Obeticholic acid can reactivate downstream FXR signaling pathway and reduces PP in the TAA and BDL (thioacetamide (TAA)-intoxicated and bile-duct–ligated) models without systemic hemodynamic impact. It also restores endothelial function and reduces the total IHVR in experimental cirrhosis

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Fiorucci S, Clerici C, Antonelli E et al. Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis. J Pharmacol Exp Ther. 2005 May;313(2):604-12. Epub 2005 Jan 11.

2. Verbeke L, Farre R, Trebicka J et al. Obeticholic acid, a farnesoid X receptor agonist, improves portal hypertension by two distinct pathways in cirrhotic rats. Hepatology. 2014 Jun;59(6):2286-98.

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