연구용제품시약 > Chemical Reagent
[APExBIO한국독점대리점] Obeticholic Acid CAS NO# 459789-99-2
바이오클론
APExBIO는 Small molecule, Inhibitor, Peptide 등의
chemical 관련 제품을 직접 생산, 공급하는 브랜드입니다.
바이오클론(주)는
APExBIO의 한국독점대리점이며,
2015년부터 정부의 화학물질의 등록 및 평가 등에
관한 법률(화평법)에 의해 모든 화학물질을 한국환경공단에
신고, 허가 하에 안전하게 수입 공급하고 있습니다.
한국환경공단 신고허가없이 수입되거나 공식대리점이 아닌 무분별한 수입업자에 공급되어진 화학물질품목은 화평법에 의해 문제소지가 발생할수 있습니다 |
Catalog No. B4888
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.
Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 420.63 |
Cas No. | 459789-99-2 |
Formula | C26H44O4 |
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 |
SDF | Download SDF |
Canonical SMILES | CCC1C2CC(CCC2(C3CCC4(C(C3C1O)CCC4C(C)CCC(=O)O)C)C)O |
Shipping Condition | Ship with blue ice, or upon other requests. |
General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
매주 금요일 4시 발주
Homepage : www.bioclone.co.kr
한국공식대리점 바이오클론㈜
T) 02-2690-0058 F) 02-2690-0397
www.bioclone.co.kr
본 정보는 "바이오클론" (으)로 문의 바랍니다.