产品说明书
Alvelestat
 |
同义名 : | AZD9668;Avelestat |
| CAS号 : | 848141-11-7 | |
| 货号 : | A301653 | |
| 分子式 : | C25H22F3N5O4S | |
| 纯度 : | 99%+ | |
| 分子量 : | 545.534 | |
| MDL号 : | MFCD26960961 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 35 mg/mL(64.16 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear PO 0.5% CMC-Na 45 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Mutations in ELANE, the gene for neutrophil elastase (NE), a protease expressed early in neutrophil development, are the most frequent cause of cyclic (CyN) and severe congenital neutropenia (SCN)[3]. Alvelestat is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM[4]. Alvelestat (20 μg/mL; 16 hours; HBE and A549 cells) treatment decreases cells death and decreases the levels of IL-1β, IL-6, and TNF-αin vitro[5]. Alvelestat (1 - 10 mg/kg; oral administration; twice daily; for 4 days; female BALB/cJBomTac mice) treatment reduces the inflammatory response to cigarette smoke as indicated by a reduction in BAL neutrophils and interleukin-1βin vivo[4]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.83mL 0.37mL 0.18mL |
9.17mL 1.83mL 0.92mL |
18.33mL 3.67mL 1.83mL |
| 参考文献 |
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