Sivelestat sodium tetrahydrate

An inhibitor of neutrophil elastase

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库存: 现货

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10mg

￥600.00

480.00

- +
50mg

￥2025.00

1620.00

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100mg

￥2962.00

2370.00

- +

已选 0 种 0 瓶

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货号: ajci23288
CAS: 201677-61-4
别名: EI546 sodium tetrahydrate; LY544349 sodium tetrahydrate; ONO5046 sodium tetrahydrate
分子式: C??H??N?NaO??S
分子量: 528.51
纯度: >98%
溶解度: DMF: 25 mg/ml,DMSO: 15 mg/ml,Ethanol: 0.3 mg/ml,PBS (pH 7.2): 2 mg/ml
储存: Store at -20°C
库存: 现货

Background

Sivelestat(ONO5046; LY544349; EI546) 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 elastase 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 (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].

Reference:

[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.