Alvelestat

Research use only, not for human use.

Alvelestat is an orally bioavailable, selective and reversible inhibitor of human neutrophil elastase (NE), with potential anti-inflammatory activity.

Avelestat, also known as AZD9668 and MPH-966, is a novel, oral inhibitor of neutrophil elastase (NE), an enzyme implicated in the signs, symptoms, and disease progression in NE-driven respiratory diseases such as bronchiectasis and chronic obstructive pulmonary disease via its role in the inflammatory process, mucus overproduction, and lung tissue damage. 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.

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.

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.

AZD-9668 | MPH966 | Alvelestat

Proteasome/Ubiquitin

Proteasome

neutrophil elastase| neutrophil elastase

Others-Field

——

848141-11-7

545.53

C25H22F3N5O4S

>98% (HPLC)

DMSO : ≥ 33 mg/mL; 60.49 mM

c1(n(c(=O)c(cc1c1n(ncc1)C)C(=O)NCc1ccc(cn1)S(=O)(=O)C)c1cc(ccc1)C(F)(F)F)C

6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-((5-(methylsulfonyl)pyridin-2-yl)methyl)-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamide

(-20℃)

With Ice Pack

≥ 2 years