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阿尔韦莱司他 /Alvelestat {[allProObj[0].p_purity_real_show]}

货号:A301653 同义名: AZD9668;Avelestat

Alvelestat is an inhibitor of neutrophil elastase (NE) with the pIC50 of 7.9.

Alvelestat 化学结构 CAS号:848141-11-7
Alvelestat 化学结构
CAS号:848141-11-7
Alvelestat 3D分子结构
CAS号:848141-11-7
Alvelestat 化学结构 CAS号:848141-11-7
Alvelestat 3D分子结构 CAS号:848141-11-7
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Alvelestat 纯度/质量文件 产品仅供科研

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Alvelestat 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].

Alvelestat 参考文献

[1]Makaryan V, Kelley ML, Fletcher B, Bolyard AA, Aprikyan AA, Dale DC. Elastase inhibitors as potential therapies for ELANE-associated neutropenia. J Leukoc Biol. 2017 Oct;102(4):1143-1151. doi: 10.1189/jlb.5A1016-445R. Epub 2017 Jul 28. PMID: 28754797; PMCID: PMC5597518.

[2]Stevens T, Ekholm K, Gränse M, Lindahl M, Kozma V, Jungar C, Ottosson T, Falk-Håkansson H, Churg A, Wright JL, Lal H, Sanfridson A. AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase. J Pharmacol Exp Ther. 2011 Oct;339(1):313-20. doi: 10.1124/jpet.111.182139. Epub 2011 Jul 26. PMID: 21791628.

[3]Li H, Zhou X, Tan H, Hu Y, Zhang L, Liu S, Dai M, Li Y, Li Q, Mao Z, Pan P, Su X, Hu C. Neutrophil extracellular traps contribute to the pathogenesis of acid-aspiration-induced ALI/ARDS. Oncotarget. 2017 Nov 28;9(2):1772-1784. doi: 10.18632/oncotarget.22744. PMID: 29416730; PMCID: PMC5788598.

Alvelestat 实验方案

计算器
存储液制备 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

Alvelestat 技术信息

CAS号848141-11-7
分子式C25H22F3N5O4S
分子量 545.534
别名 AZD9668;Avelestat
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

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

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