Ivacaftor hydrate

Name: Ivacaftor hydrate
Brand: TargetMol
SKU: T13742L
Rating: 4.5 (1 reviews)

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产品编号 T13742LCas号 1134822-07-3

别名 VX-770 hydrate

Ivacaftor hydrate is an orally bioavailable CFTR potentiator. It also is used for cystic fibrosis treatment.

还可以

产品编号 T13742L 别名 VX-770 hydrateCas号 1134822-07-3

Ivacaftor hydrate is an orally bioavailable CFTR potentiator. It also is used for cystic fibrosis treatment.

规格	价格	库存	数量
100 mg	¥ 6,998	1-2周

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生物活性

产品描述	Ivacaftor hydrate is an orally bioavailable CFTR potentiator. It also is used for cystic fibrosis treatment.
体外活性	Ivacaftor displays no significant activity against 160 targets tested including the GABAA benzodiazepine receptor. Ivacaftor enhances the chloride secretion (EC50 of 0.236 ± 0.200 μM). Compared to the F508del HBEs, it has a 10-fold shift in potency [3]. Ivacaftor (10?μM) enhances 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) obviously increases CFTR activity in W1282X-expressing cells compared to R1162X CFTR cells[2]. VX-770 increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation, in recombinant cells. VX-770 increases forskolin-stimulated IT in temperature-corrected F508del-FRT cells by appr 6-fold with an EC50 of 25 nM[4].
体内活性	In rat, Ivacaftor (1-200 mg/kg, p.o.) shows good oral bioavailability[3].
别名	VX-770 hydrate