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Sivelestat(ONO-5046)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Sivelestat(ONO-5046)图片
CAS NO:127373-66-4
包装与价格：
包装价格(元)
10mg电议
50mg电议
200mg电议

产品介绍
Sivelestat (ONO-5046) (EI546) 是人中性粒细胞弹性蛋白酶的竞争性抑制剂，IC50 为 44 nM，Ki 为 200 nM。 Sivelestat (ONO-5046) (EI546) 具有研究 COVID-19 中急性肺损伤/急性呼吸窘迫综合征或弥散性血管内凝血的潜力。
Cas No.127373-66-4
别名西维来司他; EI546; LY544349; ONO5046
化学名2-(2-(4-(pivaloyloxy)phenylsulfonamido)benzamido)acetic acid
Canonical SMILESO=C(O)CNC(C1=CC=CC=C1NS(=O)(C2=CC=C(OC(C(C)(C)C)=O)C=C2)=O)=O
分子式C20H22N2O7S
分子量434.46
溶解度≥ 43.4mg/mL in DMSO
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 44 nM

Sivelestat (ONO-5046) is a neutrophil elastase inhibitor.

Human neutrophil elastase is a protease that hydrolyzes most connective tissue components, and it has been reported to participate in the tissue injury of rheumatoid arthritis, emphysema, adult respiratory distress syndrome as well as septic shock.

In vitro: Sivelestat was found to be able to competitively inhibit the human neutrophil elastase, and it could inhibit leukocyte elastase from rat, rabbit, mouse and hamster. Whereas, sivelestat even at 100 microM could not inhibit thrombin, plasmin, trypsin, pancreas kallikrein, plasma kallikrein, chymotrypsin and cathepsin G [1].

In vivo: In animal study, 50 or 100 mg/kg sivelestat were immediately administered by i.p. injection after the surgical procedure to male Sprague-Dawley rats with bacterial infection caused by cecal ligation and puncture. Results showed that in the untreated rats, the mean arterial pressure(MAP) and glomerular filtration rate(GFR) decreased, while serum blood urea nitrogen(BUN) and neutrophil gelatinase-associated lipocalin(NGAL) levels increased. Sivelestat was found to promot the survival of the rats with sepsis, restored the impairment of MAP and GFR, and inhibited the increased BUN and NGAL levels. In addition, sivelestat could suppress the CLP-induced macrophage infiltration in the rats [2].

Clinical trial: In Japan and the Republic of Korea, sivelestat has been approved for acute lung injury, such as acute respiratory distress syndrome in patients with systemic inflammatory response syndrome [3].

References:
[1] 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.
[2] Li G,Jia J,Ji K,Gong X,Wang R,Zhang X,Wang H,Zang B.  The neutrophil elastase inhibitor, sivelestat, attenuates sepsis-related kidney injury in rats. Int J Mol Med.2016 Sep;38(3):767-75.
[3] Aikawa N,Kawasaki Y.  Clinical utility of the neutrophil elastase inhibitor sivelestat for the treatment of acute respiratory distress syndrome. Ther Clin Risk Manag.2014 Aug 5;10:621-9.