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Ivacaftor

CAS No. : 873054-44-5

MCE 国际站：Ivacaftor

产品活性：Ivacaftor (VX-770) 是一种有效可口服的 CFTR 增效剂，靶向G551D-CFTR和F508del-CFTR的EC₅₀分别为100 nM 和 25 nM。

研究领域：Membrane Transporter/Ion Channel  |  Autophagy

作用靶点：CFTR  |  Autophagy

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. Ivacaftor (10 μM) significantly increases CFTR activity in W1282X-expressing cells compared to R1162X CFTR cells. Ivacaftor shows no significant activity against 160 targets tested including the GABA_A 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. 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 I_T in temperature-corrected F508del-FRT cells by appr 6-fold with an EC₅₀ of 25 nM.

In Vivo: Ivacaftor (1-200 mg/kg, p.o.) exhibits good oral bioavailability in rat.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Membrane Transporter/Ion Channel Compound Library  |  FDA-Approved Drug Library  |  Autophagy Compound Library  |  Drug Repurposing Compound Library  |  Endocrinology Compound Library  |  Anti-COVID-19 Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Drug-Induced Liver Injury (DILI) Compound Library  |  Rare Diseases Drug Library  |  Children’s Drug Library  |  EMA-Approved Drug Library  |  Human Metabolite Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Cell Death Library  |  Bioactive Compound Library Max  |  Glibenclamide  |  Lumacaftor  |  Tezacaftor  |  CFTR(inh)-172  |  Elexacaftor  |  Ataluren  |  Glucosamine  |  SRI-41315  |  GlyH-101  |  (R)-BPO-27  |  Vanzacaftor  |  IOWH-032  |  GLPG1837  |  Nesolicaftor  |  5,​7,​4'-​Trimethoxyflavone  |  Bamocaftor  |  Cavosonstat  |  Galicaftor  |  NJH-2-057  |  PPQ-102  |  SRI-37240  |  Icenticaftor  |  Navocaftor  |  Chromanol 293B  |  Olacaftor  |  Crinecerfont hydrochloride  |  Posenacaftor sodium  |  Astressin 2B TFA

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