Ivacaftor hydrate
| CAS号 | 1134822-07-3 | 货号 | BCP14735 |
| 中文名 | Ivacaftor hydrate | ||
| 英文名 | Ivacaftor hydrate | ||
| 中文别名 | |||
| 英文别名 | VX-770 hydrate;VX 770 hydrate;VX770 hydrate;Kalydeco hydrate; | ||
| 分子式 | C24H30N2O4 | 分子量 | 410.51 |
| 生物活性 | in vitro: In recombinant cells VX-770 increased CFTR channel open probability (P(o)) in both the F508del processing mutation and the G551D gating mutation. VX-770 also increased Cl(-) secretion in cultured human CF bronchial epithelia (HBE) carrying the G551D gating mutation on one allele and the F508del processing mutation on the other allele by approximately 10-fold, to approximately 50% of that observed in HBE isolated from individuals without CF. in vivo: At day 28, in the group of subjects who received 150 mg of VX-770, the median change in the nasal potential difference (in response to the administration of a chloride-free isoproterenol solution) from baseline was -3.5 mV (range, -8.3 to 0.5; P=0.02 for the within-subject comparison, P=0.13 vs. placebo), and the median change in the level of sweat chloride was -59.5 mmol per liter (range, -66.0 to -19.0; P=0.008 within-subject, P=0.02 vs. placebo). Toxicity: Six severe adverse events occurred in two subjects (diffuse macular rash | ||
| 信号通路 | Ion Channel/Membrane Transporter | ||
| 靶 点 | CFTR | ||
结构式
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