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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Elastase-Alvelestat (AZD9668)
Alvelestat (AZD9668)

Chemical Structure : Alvelestat (AZD9668)

CAS No.: 848141-11-7

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Alvelestat (AZD9668) (AZD-9668)

货号: PC-49230Not For Human Use, Lab Use Only.

Alvelestat (AZD9668, AZD-9668) is a potent, selective and orally active inhibitor of neutrophil elastase (NE) with IC50 of 12 nM, >600-fold selective over other neutrophil-derived serine proteases.

规格 价格 库存 数量
5 mg ￥880 In stock
10 mg ￥1380 In stock
25 mg ￥2280 In stock
50 mg ￥3880 In stock
100 mg ￥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Alvelestat (AZD9668, AZD-9668) is a potent, selective and orally active inhibitor of neutrophil elastase (NE) with IC50 of 12 nM, >600-fold selective over other neutrophil-derived serine proteases.
AZD9668 inhibited plasma NE activity in zymosan-stimulated whole blood in cell-based assays.
AZD9668 inhibited NE activity on the surface of stimulated cells and in the supernatant of primed, stimulated cells in isolated human polymorphonuclear cells.
AZD9668 showed good crossover potency to NE from other species.
Oral administration of AZD9668 to mice or rats prevented human NE-induced lung injury, measured by lung hemorrhage, and an increase in matrix protein degradation products in bronchoalveolar lavage (BAL) fluid.
AZD9668 reduced the inflammatory response to cigarette smoke as indicated by a reduction in BAL neutrophils and interleukin-1β in acute smoke models.

物理化学性质&存储条件

分子量 545.537
分子式 C25H22F3N5O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-{[5-(methanesulfonyl)pyridin-2-yl]methyl}-6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide

参考文献

1. Stevens T, et al. J Pharmacol Exp Ther. 2011 Oct;339(1):313-20.

2. Kuna P, et al. Respir Med. 2012 Apr;106(4):531-9.

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