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Alvelestat

现货
Catalog No.
B1037
NE抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,560.00
Ship with 5-10 days
5mg
¥ 1,050.00
现货
10mg
¥ 1,800.00
现货
25mg
¥ 3,600.00
Ship with 5-10 days
50mg
¥ 5,900.00
Ship with 5-10 days
100mg
¥ 9,200.00
Ship with 10-15 days

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Background

Alvelestat is an orally bioavailable inhibitor of neutrophil elastase (NE) with pIC50 value of 7.9[1].

The reversible NE inhibitor, alvelestat, is developed for treating the neutrophil-driven inflammatory lung diseases such as bronchiectasis and chronic obstructive pulmonary diseas. Alvelestat shows high affinity with human NE with a Ki value of 9.4nM. It is more than 600-fold selective for human NE over other serine proteases. In the whole-blood and cell- associated and explosive-release assays, alvelestat shows pIC50 values of 7.36, 7.32 and 7.3, respectively. In the acute lung injury model, administration of alvelestat significantly reduces the levels of hemoglobin and BAL hydroxyproline induced by human NE. In the smoke-induced airway inflammation model, alvelestat reduces both BAL neutrophils and IL-1β markedly. Furthermore, alvelestat can relieve inflammation and inhibit smoke-induced increases in lavage neutrophils and macrophages in a model of chronic smoke-induced inflammation and emphysema [1].

References:
[1] Stevens T, Ekholm K, Gränse M, et al. AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase. Journal of Pharmacology and Experimental Therapeutics, 2011, 339(1): 313-320.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt545.53
Cas No.848141-11-7
FormulaC25H22F3N5O4S
Solubility≥27.3mg/mL in DMSO
Chemical Name6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-((5-(methylsulfonyl)pyridin-2-yl)methyl)-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamide
SDFDownload SDF
Canonical SMILESCC(N1C2=CC=CC(C(F)(F)F)=C2)=C(C3=CC=NN3C)C=C(C1=O)C(NCC4=NC=C(S(C)(=O)=O)C=C4)=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

Description Alvelestat是一种口服生物可利用的中性粒细胞弹性蛋白酶(NE)抑制剂,pIC50值为7.9。
靶点 NE          
IC50 (pIC50=7.9,Ki=4.9 nM)          

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