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CAS No.: 201677-61-4

Sivelestat Sodium Tetrahydrate/西维来司钠四水合物 Catalog No. CSN11933

Synonyms: EI546 sodium tetrahydrate;LY544349 sodium tetrahydrate;ONO5046 sodium tetrahydrate

Sivelestat sodium is a competitive inhibitor of human neutrophil elastase (IC50 = 44 nM; Ki=200 nM); also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse.

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技术信息

生物活性

描述Neutrophil elastase (NE) is a neutral serine protease that degrades extracellular matrix and cell surface proteins under stressed physiological conditions. Sivelestat sodium tetrahydrate is a synthetic NE inhibitor with an IC50 value of 46 ± 2 nM (24 ± 1 µg/ml) without human serum and 22.8 ± 3.3 µM (12.1 ± 1.7 µg/mL) in the presence of serum. A significant growth suppression was observed in TMK-1 cells treated with 1 µg/mL NE together with 100, 500 and 1000 µg/mL sivelestat for 48 hours. In a one-hour treatment in TMK-1 cells, NE-induced EGFR phosphorylation and ERK1/2 phosphorylation was inhibited by 100 µg/mL sivelestat. The inhibitory effects of sivelestat on neutrophil adhesion was noted in human umbilical vein endothelial cell (HUVEC) monolayers treated with 1 µg/mL sivelestat for one hour. Also in HUVEC monolayers, one-hour incubation of 50 µg/mL sivelestat significantly suppressed PAF-induced neutrophils migrating through the membrane. In a study of C57BL/6 mice, neutrophil elastase activity that was elevated by high V_T ventilation for 4 hours in both bronchoalveolar lavage fluid and serum were significantly reduced by sivelestat at 100 mg/kg and 200 mg/kg doses, which was injected 30 min before ventilation. The degree of lung myeloperoxidase (MPO) activity was also significantly reduced in high V_T-sivelestat (100 mg/kg) group compared with mice treated by high V_T alone. Mice treated with 100 mg/kg sivelestat in the high V_T developed less pulmonary inflammation than the ones without sivelestat treatment. The scores in histopathological grades of ventilator-induced lung injury were significantly lower in mice injected with 100 mg/kg sivelestat compared to those in high V_T group. Sivelestat at the dose of 100 mg/kg also decreased neutrophils and the ratio of wet-to-dry weight, a parameter of lung oedema. The level of inflammatory markers, such as IL-6 and TNF-α, was also attenuated by sivelestat treatment at 100 mg/kg.
作用机制Sivelestat sodium tetrahydrate is an intravenously active NE inhibitor that competitively binds to the target substrate of NE.

动物研究
剂量	Golden hamster: 0.03 mg/kg - 3 mg/kg^[3] (i.v.) Mice: 3 mg/kg^[4] (i.p.) Rat: 15 mg/kg, 60 mg/kg^[5] (intra-abdominally); 50 mg/kg - 100 mg/kg^[6] (i.p.)
给药途径	i.v., i.p., intra-abdominally

参考文献

[1] Yoshikawa N, Inomata T, et al. Sivelestat sodium hydrate reduces radiation-induced lung injury in mice by inhibiting neutrophil elastase. Mol Med Rep. 2013 Apr;7(4):1091-5.
[2] Yoshikawa S, Tsushima K, et al. Effects of a synthetic protease inhibitor (gabexate mesilate) and a neutrophil elastase inhibitor (sivelestat sodium) on acid-induced lung injury in rats. Eur J Pharmacol. 2010 Sep 1;641(2-3):220-5.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8921 mL
- 9.4606 mL
- 18.9211 mL
- 5 mM
- 0.3784 mL
- 1.8921 mL
- 3.7842 mL
- 10 mM
- 0.1892 mL
- 0.9461 mL
- 1.8921 mL

技术信息

CAS号

201677-61-4

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H29N2NaO11S

运输

蓝冰

分子量

528.51

别名

EI546 sodium tetrahydrate;LY544349 sodium tetrahydrate;ONO5046 sodium tetrahydrate;Sivelestat Sodium;ONO-5046 Sodium;EI-546 Sodium;LY-544349 Sodium;Sivelestat (sodium salt hydrate);LY544349;ONO-5046;西维来司钠四水合物

溶解度

DMSO	98.0 mg/mL (185.4 mM)
Water	Insoluble
Ethanol	100.0 mg/mL (189.2 mM)

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Sivelestat Sodium Tetrahydrate/西维来司钠四水合物 Catalog No. CSN11933

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