Ivacaftor benzenesulfonate

Name: Ivacaftor benzenesulfonate
Brand: TargetMol
SKU: T13742
Rating: 4.5 (1 reviews)

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产品编号 T13742Cas号 1134822-09-5

别名 VX-770 benzenesulfonate

Ivacaftor benzenesulfonate used for cystic fibrosis treatment. is an orally bioavailable CFTR potentiator.

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产品编号 T13742 别名 VX-770 benzenesulfonateCas号 1134822-09-5

Ivacaftor benzenesulfonate used for cystic fibrosis treatment. is an orally bioavailable CFTR potentiator.

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生物活性

产品描述	Ivacaftor benzenesulfonate used for cystic fibrosis treatment. is an orally bioavailable CFTR potentiator.
体外活性	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 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. 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 in temperature-corrected F508del-FRT cells by appr 6-fold with an EC50 of 25 nM.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.
体内活性	Ivacaftor (1-200 mg/kg, p.o.) exhibits good oral bioavailability in rat.
别名	VX-770 benzenesulfonate