product name Alvelestat (AZD9668)
Description: Alvelestat, also known as AZD9668, is an orally available, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, it is at least 600-fold more selective over other serine proteases. In cell-based assays, AZD9668 inhibited plasma NE activity in zymosan-stimulated whole blood. AZD9668 has the potential to reduce lung inflammation and the associated structural and functional changes in human diseases.
References: J Pharmacol Exp Ther. 2011 Oct;339(1):313-20.
545.53
Formula
C25H22F3N5O4S
CAS No.
848141-11-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (183.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
AZD9668
other peoduct :
In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
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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. |
Animal model | Human NE-induced acute lung injury in mice or rats, guinea pig chronic smoke model. |
Formulation & Dosage | Formulated in 0.5% hydroxypropyl methylcellulose in citrate buffer, 20% glucose and 0.1% polysorbate in water or corn oil; ~10 mg/kg (mice); ~20 mg/kg (rats); ~100 mg/kg (pigs); oral gavage |
References | J Pharmacol Exp Ther. 2011 Oct;339(1):313-20. |