China Wholesale Rosuvastatin Calcium 10 Suppliers - Obeticholic Acid – CPF
China Wholesale Rosuvastatin Calcium 10 Suppliers - Obeticholic Acid – CPF Detail:
Description
Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy[1][2][3].
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
- 1. Selina Costa. “Characterizing a Novel Ligand for the Farnesoid X Receptor using Transgenic Zebrafish.” University of Toronto. Jun-2018.
- 2. Kent, Rebecca. “Effects of Fenofibrate on CYP2D6 and Regulation of ANG1 and RNASE4 by the FXR Agonist Obeticholic Acid.” indigo.uic.edu.2017.
Storage
Powder |
-20°C |
3 years |
4°C |
2 years | |
In solvent |
-80°C |
6 months |
-20°C |
1 month |
Chemical structure
Related Biological Data
Related Biological Data
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We are going to make every single effort for being excellent and excellent, and accelerate our ways for standing while in the rank of international top-grade and high-tech enterprises for China Wholesale Rosuvastatin Calcium 10 Suppliers - Obeticholic Acid – CPF , The product will supply to all over the world, such as: Kazakhstan, Bangalore, Rwanda, Satisfaction and good credit to every customer is our priority. We focus on every detail of order processing for customers till they have received safe and sound products with good logistics service and economical cost. Depending on this, our products are sold very well in the countries in Africa, the Mid-East and Southeast Asia.
By Tina from Malta - 2018.07.12 12:19
We feel easy to cooperate with this company, the supplier is very responsible, thanks.There will be more in-depth cooperation.
By Anna from Kuwait - 2017.01.28 18:53