Sivelestat (ONO-5046)
(Synonyms: 西维来司他; EI546; LY544349; ONO5046) 目录号 : GC16724
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
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 127373-66-4 | SDF | |
| 别名 | 西维来司他; EI546; LY544349; ONO5046 | ||
| 化学名 | 2-(2-(4-(pivaloyloxy)phenylsulfonamido)benzamido)acetic acid | ||
| Canonical SMILES | O=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 tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3017 mL | 11.5085 mL | 23.0171 mL |
| 5 mM | 0.4603 mL | 2.3017 mL | 4.6034 mL |
| 10 mM | 0.2302 mL | 1.1509 mL | 2.3017 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet