Sivelestat sodium tetrahydrate (Synonyms: LY544349, ONO-5046) |
| Katalog-Nr.GC16898 |
Sivelestat (EI546) Natriumtetrahydrat ist ein kompetitiver Inhibitor der humanen neutrophilen Elastase mit einem IC50 von 44 nM und einem Ki von 200 nM. Sivelestat (EI546) Natriumtetrahydrat hat das Potenzial fÜr die Untersuchung von akuter Lungenverletzung/akutem Atemnotsyndrom oder disseminierter intravaskulÄrer Gerinnung bei COVID-19.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 201677-61-4
Sample solution is provided at 25 µL, 10mM.
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Sivelestat sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.IC50 value: 44 nM [1]Target: neutrophil elastaseONO-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 (ID50 = 82 micrograms/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase [1]. Sivelestat sodium hydrate is an anti-neutrophil elastase inhibitor and may be one of the treatment options for acute respiratory failure due to pneumocystis pneumonia in AIDS patients [2].
References:
[1]. Kawabata K, et al. ONO-5046, a novel inhibitor of human neutrophil elastase. Biochem Biophys Res Commun. 1991 Jun 14;177(2):814-20.
[2]. Imokawa S, et al. Acute respiratory failure due to pneumocystis pneumonia successfully treated with combined use of sivelestat sodium hydrate. Nihon Kokyuki Gakkai Zasshi. 2008 Jun;46(6):461-5.
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