Tsanangudzo

Obeticholic acid (INT-747) ine simba, inosarudza uye inobata nemuromo FXR agonist ine EC50 ye99 nM.Obeticholic acid ine anticholeretic uye anti-kuzvimba mhedzisiro.Obeticholic acid zvakare inokonzeresa autophagy [1] [2] [3].

Background

Obeticholic Acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECDCA, INT-747) ine simba uye inosarudza agonist yeFXR ine EC50 kukosha kwe99 nM [1].

Iyo farnesoid X receptor (FXR) inyukireya bile acid receptor inobatanidzwa mu bile acid homeostasis, chiropa fibrosis, hepatic uye intestinal kuzvimba uye chirwere chemoyo [2].

Obeticholic Acid ine simba uye inosarudza FXR agonist ine anticholeretic chiitiko [1].Obeticholic Acid is semisynthetic bile acid derivative uye ine simba FXR ligand.Mune estrogen-induced cholestasis rats, 6-ECDCA yakachengetedzwa kubva kune cholestasis inokonzerwa ne17α-ethynylestradiol (E217α) [2].Mu cirrhotic portal hypertension (PHT) rat modhi, INT-747 (30 mg/kg) yakadzoreredza nzira yechiratidzo yeFXR yakadzika uye yakaderedza kudzvinyirirwa kwepamhepo nekudzikisa zvachose intrahepatic vascular resistance (IHVR) pasina deleterious systemic hypotension.Ichi chiitiko chakabatanidzwa nekuwedzera kweNOS chiitiko [3].Mumuenzaniso weDahl rat wemunyu-sensitive hypertension uye insulin-resistance (IR), munyu wakanyanya (HS) kudya kwakawedzera zvakanyanya systemic blood pressure uye yakaderedzwa tishu DDAH kutaura.INT-747 yakawedzera insulin senitivity uye yakadzivisa kuderera kweDDAH kutaura [4].

References:
[1].Pellicciari R, Fiorucci S, Camaioni E, et al.6alpha-ethyl-chenodeoxycholic acid (6-ECCDA), ane simba uye anosarudza FXR agonist akapiwa anticholestatic basa.J Med Chem, 2002, 45(17): 3569-3572.
[2].Fiorucci S, Clerici C, Antonelli E, et al.Dziviriro mhedzisiro ye6-ethyl chenodeoxycholic acid, farnesoid X receptor ligand, mune 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, inovandudza portal hypertension nenzira mbiri dzakasiyana mumakonzo e cirrhotic.Hepatology, 2014, 59(6): 2286-2298.
[4].Ghebremariam YT, Yamada K, Lee JC, et al.FXR agonist INT-747 inogadzirisa kutaura kweDDAH uye inowedzera insulin senitivity mumakonzo ane munyu wakanyanya.PLoS One, 2013, 8(4): e60653.

Product Citation

• 1. Selina Costa."Kuita Novel Ligand yeFarnesoid X Receptor uchishandisa Transgenic Zebrafish."Yunivhesiti yeToronto.Jun-2018.
• 2. Kent, Rebeka."Migumisiro yeFenofibrate paCYP2D6 uye Regulation ye ANG1 uye RNASE4 neFXR Agonist Obeticholic Acid."indigo.uic.edu.2017.

Storage

Chimiro chemakemikari

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