Obeticholic acid

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Obeticholic acid Biliary cholangitis Ka Ntlong      


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Obeticholic acid (INT-747) ke agonist e matla, e khethang le ea molomo ea FXR e nang le EC50 ea 99 nM.Obeticholic acid e na le phello ea anticholeretic le e khahlanong le ho ruruha.Obeticholic acid e boetse e etsa hore motho a ikutloe a le mong [1] [2] [3].

 

Ka morao

Obeticholic Acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECDCA, INT-747) ke agonist e matla le e khethang ea FXR e nang le boleng ba EC50 ba 99 nM [1].

Farnesoid X receptor (FXR) ke receptor ea nyutlelie ea bile acid e amehang ho bile acid homeostasis, sebete fibrosis, ho ruruha ha sebete le mala le lefu la pelo [2].

Obeticholic Acid ke FXR agonist e matla le e khethang e nang le ts'ebetso ea anticholeretic [1].Obeticholic Acid ke semisynthetic bile acid e nkiloeng le FXR ligand e matla.Likhotong tsa cholestasis tse entsoeng ke estrogen, 6-ECDCA e sirelelitsoe khahlanong le cholestasis e bakoang ke 17α-ethynylestradiol (E217α) [2].Mefuteng ea litoeba tsa cirrhotic portal hypertension (PHT), INT-747 (30 mg/kg) e ile ea tsosolosa tsela ea pontšo ea FXR e theohelang tlaase le ho fokotsa khatello ea li-portal ka ho theola kakaretso ea intrahepatic vascular resistance (IHVR) ntle le ho senya systemic hypotension.Phello ena e ne e amahanngoa le ts'ebetso e eketsehileng ea eNOS [3].Moetsong oa Dahl rat oa khatello ea mali e nang le letsoai-sensitive hypertension le insulin-resistance (IR), lijo tse nang le letsoai le phahameng (HS) li ile tsa eketsa khatello ea mali ea systemic haholo le polelo ea DDAH ea lisele tse theohileng.INT-747 e matlafalitse kutloisiso ea insulin mme e thibela ho fokotseha ha polelo ea DDAH [4].

Litšupiso:
[1].Pellicciari R, Fiorucci S, Camaioni E, et al.6alpha-ethyl-chenodeoxycholic acid (6-ECCDA), FXR e matla le e khethang ea agonist e filoeng mosebetsi oa anticholestatic.J Med Chem, 2002, 45 (17): 3569-3572.
[2].Fiorucci S, Clerici C, Antonelli E, et al.Tšireletso ea 6-ethyl chenodeoxycholic acid, farnesoid X receptor ligand, ho cholestasis e bakoang ke estrogen.J Pharmacol Exp Ther, 2005, 313(2): 604-612.
[3].Verbeke L, Farre R, Trebicka J, et al.Obeticholic acid, farnesoid X receptor agonist, e ntlafatsa khatello ea mali ea portal ka litsela tse peli tse fapaneng ho likhoto tsa cirrhotic.Hepatology, 2014, 59 (6): 2286-2298.
[4].Ghebremariam YT, Yamada K, Lee JC, et al.FXR agonist INT-747 e laola polelo ea DDAH mme e ntlafatsa kutloisiso ea insulin ho likhoto tsa Dahl tse nang le letsoai le lengata.PLoS One, 2013, 8(4): e60653.

Tlhahiso ea Sehlahisoa

  • 1. Selina Costa."Ho khetholla Ligand ea Novel bakeng sa Farnesoid X Receptor e sebelisang Transgenic Zebrafish."Univesithi ea Toronto.Phup-2018.
  • 2. Kent, Rebeka."Liphello tsa Fenofibrate ho CYP2D6 le Taolo ea ANG1 le RNOSE4 ke FXR Agonist Obeticholic Acid."indigo.uic.edu.2017.

 

Polokelo

Phofo

-20°C

3 lilemo
 

4°C

lilemo tse 2
Ka solvent

-80°C

Likhoeli tse 6
 

-20°C

1 khoeli

Sebopeho sa lik'hemik'hale

Obeticholic Acid

Lintlha tse amanang le Biological

Obeticholic Acid2

Lintlha tse amanang le Biological

Obeticholic Acid3

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