货号:A310710
同义名:
ONO5046;LY544349
Sivelestat是人类中性粒细胞弹性蛋白酶的竞争性抑制剂(IC50 = 44 nM,Ki = 200 nM),同时也抑制从兔、鼠、仓鼠和小鼠中提取的白细胞弹性蛋白酶。
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描述 | Human neutrophil elastase (HNE) is a protease that participates in tissue injuries of emphysema, rheumatoid arthritis, and septic shock. Sivelestat is a potent, selective, intravenously active HNE inhibitor with an IC50 value of 44±3nM and a Ki value of 200±20nM. It also inhibited leukocyte elastase obtained from rabbits, rats, hamsters, and mice with IC50 values of 36±1, 19±1, 37±4, and 49±5nM, respectively. Sivelestat inhibited porcine pancreas elastase with an IC50 value of 5.6±0.2μM. Intratracheal administration of sivelestat dose-dependently suppressed lung hemorrhage in hamsters with an ID50 value of 82μg/kg. In Guinea pigs, intravenous administration of sivelestat significantly and dose-dependently suppressed HNE-induced increase in skin capillary permeability with an ID50 value of 9.6mg/kg[3]. In rats, intravenous injection of sivelestat at a dosage of 10mg/kg significantly ameliorated lung injury induced by hemorrhagic shock followed by resuscitation[4]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.30mL 0.46mL 0.23mL |
11.51mL 2.30mL 1.15mL |
23.02mL 4.60mL 2.30mL |
CAS号 | 127373-66-4 |
分子式 | C20H22N2O7S |
分子量 | 434.463 |
别名 | ONO5046;LY544349;EI546 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Sealed in dry,2-8°C |
溶解方案 |
DMSO: 105 mg/mL(241.68 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 无水乙醇: 2.5 mg/mL(5.75 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |
5% DMSO+40% PEG 300+5% Tween 80+water 23 mg/mL |