N''-[N-METHOXYCARBONYL-L-VALYL]-N-[(S)-3,3,3-TRIFLUOR-1-ISOPROPYL-2-OXOPROPYL]-L-PROLINAMIDE

Uses

ZD8321 is a potent inhibitor of human Neutrophil elastase (NE) with a Ki of 13±1.7 nM.

Biological Activity

ZD8321 is a potent inhibitor of human Neutrophil elastase (NE) with a Ki value of 13±1.7 nM.

in vitro

TNFα-activated HUVEC is dose dependently inhibited by ZD8321.The adhesion between cancer cells with high elastase activity and TNFα-activated HUVEC is also inhibited by ZD8321.

target

References

[1] Veale CA, et al. Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase. J Med Chem. 1997 Sep 26;40(20):3173-81. DOI:10.1021/jm970250z
[2] Nozawa F, et al. Elastase activity enhances the adhesion of neutrophil and cancer cells to vascular endothelial cells. J Surg Res. 2000 Dec;94(2):153-8. DOI:10.1006/jsre.2000.6002