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.

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

Soluble in DMSO > 10 mM

neutrophil elastase ,neutrophil elastase

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 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.

1. Stevens T, et al. J Pharmacol Exp Ther. 2011, 339(1), 313-320.

2. Kuna P, et al. Respir Med. 2012 Apr;106(4):531-9.