| 名称 | Sivelestat sodium tetrahydrate |
| 描述 | Sivelestat sodium tetrahydrate (ONO5046 sodium tetrahydrate) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium tetrahydrate has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19. |
| 体外活性 | Sivelestat (ONO-5046) is not an inhibitor of trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin, or cathepsin G, even at concentrations up to 100 μM[1]. However, it effectively inhibits neutrophil elastase across various species, demonstrating IC50 values of 44 nM (human), 36 nM (rabbit), 19 nM (rat), 37 nM (hamster), and 49 nM (mouse), showcasing its specificity and potential for therapeutic applications[1]. |
| 体内活性 | Sivelestat (ONO-5046, 0.021-2.1 mg/kg, intratracheally) suppresses lung hemorrhage in hamsters (ID50 = 82 pg/kg) and increases skin capillary permeability in guinea pigs (ID50 = 9.6 mg/kg) via intravenous administration, both induced by human neutrophil elastase[1]. Additionally, Sivelestat (10 mg/kg, tail vein infusion) ameliorates lung injury after hemorrhagic shock in rats[2], and prevents ischemia-reperfusion injury in the rat bladder (15, 60 mg/kg, ip)[3]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 225 mg/mL (425.7 mM), Sonication is recommended.
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| 关键字 | ONO-5046 sodium Tetrahydrate | Elaspol sodium | ONO5046 sodium | Sivelestat sodium | ONO5046 sodium Tetrahydrate | ONO-5046 sodium | Elaspol sodium Tetrahydrate | Sivelestat sodium Tetrahydrate |
| 相关产品 | PMSF | Nafamostat mesylate | Diminazene Aceturate | AEBSF hydrochloride | Leupeptin Hemisulfate | 2-(2-bromophenyl)-5-chloro-4H-3,1-benzoxazin-4-one | Ceritinib | Aprotinin | 2,4-Dioxaspiro(5.5)undec-8-ene, 3-(2-furanyl)- | Benzamidine hydrochloride |
| 相关库 | FDA上市及药典收录分子库 | 经典已知活性库 | 上市药物库 | 药物功能重定位化合物库 | 抗病毒库 | 抑制剂库 | 已知活性化合物库 |
United States
