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      Ivacaftor (hydrate)研究進(jìn)展

      發(fā)布日期:2017-11-01   瀏覽次數(shù):0
      核心提示:a href=https://www.medchemexpress.com/ivacaftor-hydrate.htmlIvacaftor (hydrate)/a產(chǎn)品描述:Ivacaftor hydrate is an orall
      Ivacaftor (hydrate)產(chǎn)品描述:Ivacaftor hydrate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.In Vitro: Ivacaftor (10 µM) increases the PC secretion activity by 3-fold for ABCB4-G535D, 13.7-fold for ABCB4-G536R, 6.7-fold for ABCB4-S1076C, 9.4-fold for ABCB4-S1176L, and 5.7-fold for ABCB4-G1178S. Ivacaftor corrects the functional defect of ABCB4 mutants[1]. Ivacaftor (10 μM) significantly increases CFTR activity in W1282X-expressing cells compared to R1162X CFTR cells[2]. Ivacaftor shows no significant activity against 160 targets tested including the GABAA benzodiazepine receptor. Ivacaftor increases the chloride secretion with an EC50 of 0.236 ± 0.200 μM, a 10-fold shift in potency compared to the F508del HBEs[3]. In recombinant cells, VX-770 increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation. VX-770 increases forskolin-stimulated IT

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      產(chǎn)品鏈接:www.medchemexpress.cn/ivacaftor-hydrate.html

       
       
       
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