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西维来司钠四水合物 /Sivelestat Sodium Tetrahydrate {[allProObj[0].p_purity_real_show]}

货号:A274870 同义名: ONO5046 sodium tetrahydrate;EI546 sodium tetrahydrate Ambeed 开学季,买赠积分,赢豪礼

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.

Sivelestat Sodium Tetrahydrate 化学结构 CAS号:201677-61-4
Sivelestat Sodium Tetrahydrate 化学结构
CAS号:201677-61-4
Sivelestat Sodium Tetrahydrate 3D分子结构
CAS号:201677-61-4
Sivelestat Sodium Tetrahydrate 化学结构 CAS号:201677-61-4
Sivelestat Sodium Tetrahydrate 3D分子结构 CAS号:201677-61-4
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Sivelestat Sodium Tetrahydrate 纯度/质量文件 产品仅供科研

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Sivelestat Sodium Tetrahydrate 生物活性

描述 Sivelestat (EI546) sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM.This compound is under investigation for its potential use in the treatment of acute lung injury/acute respiratory distress syndrome (ALI/ARDS) or disseminated intravascular coagulation (DIC), particularly in the context of COVID-19[1].[2].[3].[4].
体内研究

When administered intratracheally at dosages ranging from 0.021 to 2.1 mg/kg, Sivelestat significantly suppresses lung hemorrhage in hamsters (ID50 = 82 pg/kg) and reduces the increase of skin capillary permeability in guinea pigs (ID50 = 9.6 mg/kg), both of which are induced by human neutrophil elastase[1].

Additionally, the compound, when infused via the tail vein at a dose of 10 mg/kg, has been shown to ameliorate lung injury following hemorrhagic shock in rats[2].

Furthermore, at doses of 15 and 60 mg/kg administered intraperitoneally, Sivelestat effectively prevents ischemia-reperfusion injury in the rat bladder[3].

体外研究

Sivelestat (also known as ONO-5046) does not inhibit a range of other proteases including trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin, and cathepsin G, even at concentrations as high as 100 μM[1].

Sivelestat exhibits IC50 values ranging from 19 nM to 49 nM against neutrophil elastase derived from various species including humans, rabbits, rats, hamsters, and mice, indicating its broad efficacy across species[1].

作用机制 Sivelestat sodium tetrahydrate is an intravenously active NE inhibitor that competitively binds to the target substrate of NE.

Sivelestat Sodium Tetrahydrate 动物研究

Dose 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.)
Administration i.v., i.p., intra-abdominally

Sivelestat Sodium Tetrahydrate 参考文献

[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]Yuichiro Toda, et al. A neutrophil elastase inhibitor, sivelestat, ameliorates lung injury after hemorrhagic shock in rats. Int J Mol Med. 2007 Feb;19(2):237-43.

[3]Tomoharu Kono, et al. Neutrophil elastase inhibitor, sivelestat sodium hydrate prevents ischemia-reperfusion injury in the rat bladder. Mol Cell Biochem. 2008 Apr;311(1-2):87-92.

[4]Adeleh Sahebnasagh, et al. Neutrophil elastase inhibitor (sivelestat) may be a promising therapeutic option for management of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19. J Clin Pharm Ther. 2

Sivelestat Sodium Tetrahydrate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.46mL

1.89mL

0.95mL

18.92mL

3.78mL

1.89mL

Sivelestat Sodium Tetrahydrate 技术信息

CAS号201677-61-4
分子式C20H29N2NaO11S
分子量 528.51
别名 ONO5046 sodium tetrahydrate;EI546 sodium tetrahydrate;ONO-5046;LY544349;Sivelestat (sodium salt hydrate);LY544349 sodium;EI546 sodium;Sodium sivelestat;ONO5046-Na;Sivelestat sodium;LY544349 sodium tetrahydrate
运输蓝冰
存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 250 mg/mL(473.03 mM),配合低频超声助溶,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

动物实验配方
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