Alvelestat
| CAS号 | 848141-11-7 | 货号 | BCP07945 |
| 中文名 | Alvelestat | ||
| 英文名 | Alvelestat | ||
| 中文别名 | |||
| 英文别名 | AZD9668;AZD-9668;AZD 9668; | ||
| 分子式 | C25H22F3N5O4S | 分子量 | 545.53 |
| 生物活性 | in vitro: AZD9668 had a high binding affinity for human NE (KD = 9.5 nM) and potently inhibited NE activity. The calculated pIC50 (IC50) and Ki values for AZD9668 for human NE were 7.9 (12 nM) and 4.9 nM, respectively. In contrast to earlier NE inhibitors, the interaction between AZD9668 and NE was rapidly reversible. AZD9668 was also highly selective for NE over other neutrophil-derived serine proteases. In cell-based assays, AZD9668 inhibited plasma NE activity in zymosan-stimulated whole blood. In isolated human polymorphonuclear cells, AZD9668 inhibited NE activity on the surface of stimulated cells and in the supernatant of primed, stimulated cells.AZD9668 showed good crossover potency to NE from other species. in vivo: Six hundred and fifteen patients were randomised: placebo (302), AZD9668 60 mg bid (313). AZD9668 showed no effect on lung function: change in mean pre-bronchodilator FEV1 versus placebo was 0.01L (95% confidence interval: -0.03, 0.05; p=0.533). AZD9668 did not sig | ||
| 信号通路 | Protease/Metabolic Enzyme | ||
| 靶 点 | Elastase | ||
结构式
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