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Alvelestat

In stock
Catalog No.
B1037
NE inhibitor
Grouped product items
SizePriceStock Qty
100mg
$920.00
In stock

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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
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description Alvelestat is an orally bioavailable inhibitor of neutrophil elastase (NE) with pIC50 value of 7.9
Targets NE          
IC50 (pIC50=7.9,Ki=4.9 nM)          

Quality Control

Chemical structure

Alvelestat