Ivacaftor依伐卡托,873054-44-5

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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.

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