China Wholesale Rosuvastatin Manufacturer Suppliers - Obeticholic Acid – CPF

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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

Obeticholic Acid

Related Biological Data

Obeticholic Acid2

Related Biological Data

Obeticholic Acid3

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

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Proposal 18 Quality Consistency Evaluation projects which have approved 4, and 6 projects are under approving.

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We're proud from the higher client fulfillment and wide acceptance due to our persistent pursuit of high quality both on product and service for China Wholesale Rosuvastatin Manufacturer Suppliers - Obeticholic Acid – CPF , The product will supply to all over the world, such as: Japan, Islamabad, Zambia, Our products have won an excellent reputation at each of the related nations. Because the establishment of our firm. we've insisted on our production procedure innovation together with the most recent modern day managing method, attracting a sizable quantity of talents within this industry. We regard the solution good quality as our most vital essence character.
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