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Description: Sivelestat sodium, the sodium salt of Sivelestat (also known as ONO5046; LY544349; EI546), is a novel, potent and competitive inhibitor of human neutrophil elastase (HNE) with IC50 value of 44 nM and Ki of 200 nM; it also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse. ONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 microM. In in vivo studies, ONO-5046 suppressed lung hemorrhage in hamster by intratracheal administration and increase of skin capillary permeability in guinea pig by intravenous administration. It is used in the treatment of acute respiratory failure. Preliminary studies show Sivelestat may also improve neuropathic pain.
References: Interact Cardiovasc Thorac Surg. 2008 Oct; 7(5):785-8; Dig Dis Sci. 2014 Apr; 59(4):787-94.
Related CAS#:201677-61-4 (Sivelestat sodium tetrahydrate); 127373-66-4 (free acid)
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