China Best-Selling Sofosbuvir Daclatasvir - Obeticholic Acid – CPF manufacturers and suppliers

Best-Selling Sofosbuvir Daclatasvir - Obeticholic Acid – CPF

Short Description:

Product Detail

Product Tags

Feedback (2)

"Control the standard by the details, show the toughness by quality". Our firm has strived to establish a highly efficient and stable workers workforce and explored an effective high-quality management system for Doxycycline Hyclate 100 Mg Oral Capsule, Sacubitril Manufacturer, Is Hydrochlorothiazide, Leading the trend of this field is our persistent goal. Providing first class products is our aim. To create a beautiful future, we would like to cooperate with all friends at home and abroad. Should you have any interest in our products, please do not hesitate to contact us.

Best-Selling Sofosbuvir Daclatasvir - 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