Sivelestat sodium (201677-61-4) is a potent and selective leukocyte elastase inhibitor, IC50 = 44 nM.1 Displays no activity at a variety of other proteases. Inhibits NF-κB activation leading to decreased serum cytokine levels2 and LTB4-induced neutrophil migration in vitro3. Significantly attenuates ischemia-induced spinal cord injury4 and reduces acute inflammatory lung injury in vivo5.
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
5) Iwata et al. (2010), Effect of neutrophil elastase inhibitor (sivelestat sodium) in the treatment of acute lung injury (ALI) and acute respiratory distress syndrome (ARDS): a systemic review and meta-analysis; Intern. Med., 49 2423