Bayani

Obeticolic acid (INT-747) mai ƙarfi ne, zaɓaɓɓe kuma mai aiki da baki agonist FXR tare da EC50 na 99 nM.Obeticolic acid yana da tasirin anticholeretic da anti-kumburi.Obeticolic acid kuma yana haifar da autophagy [1] [2] [3].

Fage

Obeticolic Acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECDCA, INT-747) shine mai ƙarfi kuma zaɓi agonist na FXR tare da ƙimar EC50 na 99 nM [1].

Mai karɓar farnesoid X (FXR) shine mai karɓar bile acid na nukiliya wanda ke cikin bile acid homeostasis, fibrosis hanta, kumburin hanta da na hanji da cututtukan zuciya [2].

Obeticholic acid ne mai ƙarfi kuma zaɓin FXR agonist tare da aikin anticholeretic [1].Obeticholic acid wani nau'in bile acid ne na semisynthetic kuma mai ƙarfi FXR ligand.A cikin berayen cholestasis na estrogen-induced, 6-ECDCA an kiyaye shi daga cholestasis wanda 17a-ethynylestradiol (E217a) [2] ya haifar.A cikin nau'ikan bera na cirrhotic portal hypertension (PHT), INT-747 (30 mg/kg) ya sake kunna hanyar siginar FXR na ƙasa da rage matsa lamba ta hanyar rage jimlar juriya na jijiyoyin bugun jini (IHVR) ba tare da ƙarancin hauhawar jini ba.Wannan tasirin yana da alaƙa da haɓaka ayyukan eNOS [3].A cikin samfurin Dahl rat na hauhawar hauhawar jini mai saurin gishiri da juriya na insulin (IR), babban abinci mai gishiri (HS) yana ƙaruwa da haɓakar hawan jini na tsarin jiki da ƙarancin tsarin DDAH nama.INT-747 yana haɓaka ƙwarewar insulin kuma ya hana raguwar maganganun DDAH [4].

Magana:
[1].Pellicciari R, Fiorucci S, Camaioni E, et al.6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), mai ƙarfi da zaɓi na FXR agonist wanda aka ba shi aikin anticholestatic.J Med Chem, 2002, 45 (17): 3569-3572.
[2].Fiorucci S, Clerici C, Antonelli E, et al.Tasirin kariya na 6-ethyl chenodeoxycholic acid, farnesoid X ligand mai karɓa, a cikin cholestasis mai haifar da isrogen.J Pharmacol Exp Ther, 2005, 313 (2): 604-612.
[3].Verbeke L, Farre R, Trebicka J, et al.Obeticholic acid, farnesoid X agonist mai karɓa, yana haɓaka hawan jini ta portal ta hanyoyi guda biyu daban-daban a cikin berayen cirrhotic.Hepatology, 2014, 59 (6): 2286-2298.
[4].Ghebremariam YT, Yamada K, Lee JC, et al.FXR agonist INT-747 yana haɓaka maganganun DDAH kuma yana haɓaka haɓakar insulin a cikin berayen Dahl da ake ciyar da gishiri mai girma.PLoS Daya, 2013, 8 (4): e60653.

Bayanin Samfura

• 1. Selina Costa."Haɓaka wani Novel Ligand don Mai karɓar Farnesoid X ta amfani da Zebrafish Transgenic."Jami'ar Toronto.Juni-2018.
• 2. Kent, Rebecca."Tasirin Fenofibrate akan CYP2D6 da Tsarin ANG1 da RNASE4 ta FXR Agonist Obeticholic Acid."indigo.uic.edu.2017.

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