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Ivacaftor 结构式

依伐卡托

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货号 :BCP01857CAS号 :873054-44-5纯度:98%
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  • 基本信息与产品描述
CAS号 873054-44-5 货号 BCP01857
中文名 依伐卡托
英文名 Ivacaftor
中文别名
英文别名 VX-770;VX770;VX 770;Kalydeco;
SMILES
化学名称
分子式 C24H28N2O3 分子量 392.49
纯度 98% 配送 惯例下常温包邮
产品描述 Ivacaftor (10 μM) significantly increases the forskolin-stimulated Cl- secretion (IT) by ~4-fold with an EC50 of 100 nM in the recombinant Fisher rat thyroid (FRT) cells expressing G551D gating mutation of CFTR, and by ~6-fold with an EC50 of 25 nM in the recombinant cells expressing temperature-corrected F508del processing mutation of CFTR. Consistent with the increases in the forskolin-stimulated IT, Ivacaftor (10 μM) increases the open probability (Po) of G551D-, F508del-, and wild-type CFTR by ~6-fold, ~5-fold and ~2-fold, respectively, indicating that Ivacaftor acts directly on CFTR to increase its gating activity. In primary cultured human CF bronchial epithelia (HBE) carrying the G551D and F508del CFTR mutations, Ivacaftor (10 μM) potently increases the forskolin-stimulated IT by ~10-fold from 5% to a maximum level of 48% of that measured in non-CF HBE, with an EC50 of 236 nM displaying ~70-fold more potency compared with the commonly used CFTR potentiator genistein, which has a
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