APExBIO는 Small molecule, Inhibitor, Peptide 등의
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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 .
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 .
Obeticholic Acid is a potent and selective FXR agonist with anticholeretic activity . 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) . 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 . 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 .
. 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.
. 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.
. 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.
. 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.
||Store at -20°C
||≥21.5 mg/mL in DMSO; insoluble in H2O; ≥21.3 mg/mL in EtOH
||Ship with blue ice, or upon other requests.
||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.
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