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Sivelestat sodium tetrahydrate (Synonyms: LY544349, ONO-5046)

カタログ番号GC16898

シベレスタット (EI546) ナトリウム四水和物は、ヒト好中球エラスターゼの競合阻害剤であり、IC50 は 44 nM、Ki は 200 nM です。シベレスタット (EI546) 四水和物ナトリウムは、COVID-19 における急性肺損傷/急性呼吸窮迫症候群または播種性血管内凝固症候群の研究の可能性を秘めています。

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Sivelestat sodium tetrahydrate 化学構造

Cas No.: 201677-61-4

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10mg
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50mg
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100mg
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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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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