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Ivacaftor hydrate is an orally bioavailable CFTR potentiator. It also is used for cystic fibrosis treatment.
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 |
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 |
分子量 | 410.514 |
分子式 | C24H30N2O4 |
CAS No. | 1134822-07-3 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
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