Kev piav qhia

Obeticholic acid (INT-747) yog lub zog, xaiv thiab hais lus FXR agonist nrog EC50 ntawm 99 nM. Obeticholic acid muaj cov nyhuv anticholeretic thiab tiv thaiv kab mob. Obeticholic acid kuj induces autophagy[1][2][3].

Keeb kwm

Obeticholic Acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECDCA, INT-747) yog lub zog thiab xaiv agonist ntawm FXR nrog EC50 tus nqi ntawm 99 nM [1].

Farnesoid X receptor (FXR) yog ib tug nuclear bile acid receptor koom nrog hauv cov kua tsib acid homeostasis, daim siab fibrosis, kab mob siab thiab plab hnyuv thiab kab mob plawv [2].

Obeticholic Acid yog ib qho muaj zog thiab xaiv FXR agonist nrog kev ua haujlwm anticholeretic [1]. Obeticholic Acid yog semisynthetic bile acid derivative thiab muaj zog FXR ligand. Hauv estrogen-induced cholestasis nas, 6-ECDCA tiv thaiv cholestasis induced los ntawm 17α-ethynylestradiol (E217α) [2]. Nyob rau hauv cirrhotic portal hypertension (PHT) nas qauv, INT-747 (30 mg / kg) reactivated FXR downstream signaling pathway thiab txo portal siab los ntawm txo tag nrho intrahepatic vascular resistance (IHVR) yam tsis muaj deleterious systemic hypotension. Cov txiaj ntsig no tau cuam tshuam nrog nce eNOS kev ua haujlwm [3]. Hauv Dahl nas qauv ntawm ntsev-rhiab siab kub siab thiab insulin-tiv taus (IR), ntsev siab (HS) kev noj zaub mov ua rau cov ntshav siab thiab cov ntaub so ntswg downregulated DDAH. INT-747 txhim kho insulin rhiab heev thiab inhibited qhov txo qis ntawm DDAH qhia [4].

Cov ntaub ntawv:
[1]. Pellicciari R, Fiorucci S, Camaioni E, et al. 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), muaj zog thiab xaiv FXR agonist tau txais txiaj ntsig nrog kev ua haujlwm anticholestatic. J Med Chem, 2002, 45(17): 3569-3572.
[2]. Fiorucci S, Clerici C, Antonelli E, thiab al. Kev tiv thaiv los ntawm 6-ethyl chenodeoxycholic acid, farnesoid X receptor ligand, hauv cov tshuaj estrogen-induced cholestasis. J Pharmacol Exp Ther, 2005, 313(2): 604-612.
[3]. Verbeke L, Farre R, Trebicka J, et al. Obeticholic acid, farnesoid X receptor agonist, txhim kho portal hypertension los ntawm ob txoj hauv kev hauv cov nas cirrhotic. Hepatology, 2014, 59(6): 2286-2298.
[4]. Ghebremariam YT, Yamada K, Lee JC, et al. FXR agonist INT-747 upregulates DDAH qhia thiab txhim kho cov tshuaj insulin rhiab heev hauv cov ntsev noj Dahl nas. PLoS Ib, 2013, 8(4): e60653.

Khoom Citation

• 1. Selina Costa. "Tus cwj pwm tshiab Ligand rau Farnesoid X Receptor siv Transgenic Zebrafish." University of Toronto. Jun-2018.
• 2. Kent, Rebecca Pub. "Cov teebmeem ntawm Fenofibrate ntawm CYP2D6 thiab Kev Cai ntawm ANG1 thiab RNASE4 los ntawm FXR Agonist Obeticholic Acid." indigo.uic.edu.2017.

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Cov ntaub ntawv ntsig txog Biological

Cov ntaub ntawv ntsig txog Biological