For research use only. Not for use in humans.
Catalog No.S7218 Synonyms: Avelestat
Molecular Weight(MW): 545.53
Alvelestat (AZD9668) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases. Phase 2.
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Choose Selective Serine Protease Inhibitors
|Description||Alvelestat (AZD9668) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases. Phase 2.|
AZD9668 inhibits plasma NE activity in zymosan-stimulated whole blood, and also inhibits NE activity on the surface of stimulated polymorphonuclear cells and in the supernatant of primed, stimulated cells. 
|In vivo||In mice and rats, AZD9668 (p.o.) prevents human NE-induced lung injury. In a mouse model of smoke-induced airway inflammation, AZD9668 significantly reduces the number of BAL neutrophils and BAL IL-1β. In a guinea pig chronic smoke model, AZD9668 prevents airspace enlargement and small airway wall remodeling in guinea pigs in response to chronic tobacco smoke exposure. |
|In vitro||DMSO||100 mg/mL (183.3 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02669251||Recruiting||Drug: MPH966||Chronic Graft vs Host Disease|Chronic Graft-Versus-Host-Disease|Bronchiolitis Obliterans Syndrome||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||April 28 2016||Phase 1|Phase 2|
|NCT01214122||Withdrawn||Drug: AZD9668|Drug: Warfarin||Pharmacokinetics|Pharmacodynamics||AstraZeneca||November 2010||Phase 1|
|NCT01161355||Completed||Drug: AZD9668||Healthy||AstraZeneca||June 2010||Phase 1|
|NCT01147549||Completed||Drug: [C14]AZD9668||Healthy||AstraZeneca||June 2010||Phase 1|
|NCT01035411||Completed||Drug: AZD9668||Chronic Obstructive Pulmonary Disease||AstraZeneca||November 2009||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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