Sivelestat (127373-66-4) is a potent and selective leukocyte elastase inhibitor, IC50 = 44 nM1. Displays no activity at a variety of other proteases. Inhibits NF-κB activation2 and LTB4-induced neutrophil migration in vitro3. Sivelestat significantly attenuates ischemia-induced spinal cord injury, decreases serum cytokine levels and reduces acute inflammatory lung injury in vivo4.
1) Kawabata et al. (1991), ONO-5046, a novel inhibitor of human neutrophil elastase; Biochem. Biophys. Res. Commun., 177 814
2) Hagiwara et al. (2009), Neutrophil elastase inhibitor (sivelestat) reduces the levels of inflammatory mediators by inhibiting NFκB; Inflamm. Res., 58 198
3) Young et al. (2007), Role of neutrophil elastase in LTB4-induced neutrophil transmigration in vivo assessed with a specific inhibitor and neutrophil elastase deficient mice; Br. J. Phamracol., 151 628
4) Iwamoto et al. (2009), Protective effect of sivelestat sodium hydrate (ONO-5046) on ischemic spinal cord injury; Interact. Cardiovasc. Thorac. Surg., 8 606