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Sivelestat

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Chemical Structure| 127373-66-4 同义名 : ONO5046;LY544349;EI546
CAS号 : 127373-66-4
货号 : A310710
分子式 : C20H22N2O7S
纯度 : 98%
分子量 : 434.463
MDL号 : MFCD00889071
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：

5% DMSO+40% PEG 300+5% Tween 80+water 23 mg/mL

生物活性
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].
实验方案
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
参考文献

[1]Li G, Jia J, et al. The neutrophil elastase inhibitor, sivelestat, attenuates sepsis-related kidney injury in rats. Int J Mol Med. 2016 Sep;38(3):767-75.

[2]Imokawa S, Mori K, 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. Japanese.

[3]Kawabata K, Suzuki M, Sugitani M, Imaki K, Toda M, Miyamoto T. ONO-5046, a novel inhibitor of human neutrophil elastase. Biochem Biophys Res Commun. 1991 Jun 14;177(2):814-20.

[4]Toda Y, Takahashi T, Maeshima K, Shimizu H, Inoue K, Morimatsu H, Omori E, Takeuchi M, Akagi R, Morita K. A neutrophil elastase inhibitor, sivelestat, ameliorates lung injury after hemorrhagic shock in rats. Int J Mol Med. 2007 Feb;19(2):237-43.