Molecular Formula | C25H22F3N5O4S
|
Molar Mass | 545.53 |
Density | 1.42±0.1 g/cm3(Predicted) |
Melting Point | 207-209°C |
Boling Point | 780.4±60.0 °C(Predicted) |
Solubility | 25°C: DMSO |
Appearance | Solid |
Color | White |
pKa | 11.00±0.20(Predicted) |
Storage Condition | -20°C Freezer |
Use | Alvelestat (AZD9668) is an orally available, highly selective neutrophil elastase (NE) inhibitor with IC50 and Ki of 12 nM and 9.4 nM respectively, and its selectivity is at least 600 times higher than other serine proteases. |
In vitro study | AZD9668 inhibits plasma NE activity in whole blood stimulated by zymosan, and AZD9668 also inhibits NE activity in supernatants in which stimulated cells have been exposed to antigen and on the surface of stimulated Polymorphonuclear cells. |
In vivo study | In mice and rats, AZD9668 (oral) prevented lung injury of human NE induction. AZD9668 significantly reduced the number of BAL neutrophils and BAL IL-1β in a mouse model of smoke-induced airway inflammation. In a guinea pig model of long-term exposure to smoke, AZD9668 prevented spatial enlargement and small airway wall remodeling. |