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生物活性
Sivelestat sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase (HNE) (IC50 = 44 nM, Ki = 0.2 µM). Sivelestat sodium tetrahydrate also effectively inhibits leukocyte elastase derived from hamster, mouse, rabbit and rat (IC50 = 19 to 49 nM). Sivelestat sodium tetrahydrate, even at concentrations of 100 µM, does not inhibit plasma kallikrein, plasmin, thrombin, trypsin, pancreas kallikrein, chymotrypsin and cathepsin G.
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体外研究
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体内研究
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激酶实验
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细胞实验
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动物实验
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不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
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例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。
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参考文献
[1] Maeda, Y. et al.,, Sivelestat Relaxes Porcine Coronary Artery via Inhibition of Ca2+ Sensitization Induced by a Receptor Agonist. J. Cardiovasc. Pharmacol. 51, 476-482, (2008)
[2] Shimoda, M. et al.,, Protective effect of Sivelestat in a porcine hepatectomy model prepared using an intermittent Pringle method. Eur. J. Pharmacol. 587, 248-252, (2008)
[3] Kono, T. et al.,, Neutrophil elastase inhibitor, sivelestat sodium hydrate prevents ischemia-reperfusion injury in the rat bladder. Mol. Cell Biochem. 311, 87-92, (2008)
分子式
C20H29N2NaO11S |
分子量
528.51 |
CAS号
201677-61-4 |
储存方式
-20 ℃长期冷藏储存。冰袋运输 |
溶剂（常温）
|
DMSO
100 mg/mL |
Water
<1 mg/mL |
Ethanol
100 mg/mL |
体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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