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Chemical Structure : Alvelestat (AZD9668)
CAS No.: 848141-11-7
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
| 100 mg | $758 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 545.537 | |
| Formula | C25H22F3N5O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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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