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Alvelestat NE inhibitor

Catalog No.B1037
Size Price Stock Qty
100mg
$920.00
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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Alvelestat

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)          

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Chemical Properties

Cas No. 848141-11-7 SDF Download SDF
Chemical Name 6-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
Canonical SMILES CC(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
Formula C25H22F3N5O4S M.Wt 545.53
Solubility >27.3mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For 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.

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.