Alvelestat (AZD9668) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM.
体外研究
Alvelestat (20 μg/mL; 16 hours; HBE and A549 cells) treatment decreases cells death and decreases the levels of IL-1β, IL-6, and TNF-α in vitro.
Cell Viability Assay
Cell Line:
Human bronchial epithelial cells (HBE) and human alveolar epithelial cells (A549)
Concentration:
20 μg/mL
Incubation Time:
16 hours
Result:
Decreased cytotoxicity and inflammatory responses.
体内研究
Alvelestat (1-10 mg/kg; oral administration; twice daily; for 4 days; Female BALB/cJBomTac mice) treatment reduces the inflammatory response to cigarette smoke as indicated by a reduction in BAL neutrophils and interleukin-1β.
Animal Model:
Female BALB/cJBomTac mice exposed to smoke cigarette smoke
Dosage:
1 mg/kg , 3 mg/kg , 6 mg/kg , 10 mg/kg
Administration:
Oral administration; twice daily; for 4 days
Result:
Reduced the inflammatory response to cigarette smoke as indicated by a reduction in BAL neutrophils and interleukin-1β.
分子式
C25H22F3N5O4S
分子量
545.53
CAS号
848141-11-7
运输条件
Room temperature in continental US; may vary elsewhere.