西维来司钠四水合物 T20762

Product Introduction
Bioactivity


英文名: Sivelestat sodium tetrahydrate

描述: Sivelestat sodium tetrahydrate (ONO5046 sodium tetrahydrate) 是竞争性的人类中性粒细胞弹性蛋白酶的抑制剂，其 IC50 值为 44 nM， Ki 值为 200 nM。Sivelestat (EI546) sodium tetrahydrate 有潜力用于 COVID-19的急性肺损伤/急性呼吸窘迫综合征或弥散性血管内凝血的研究。

体外活性: Sivelestat (ONO-5046) does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM[1]. Sivelestat (ONO-5046) exhibits IC50 values of 44 nM, 36 nM, 19 nM, 37 nM and 49 nM for human, rabbit, rat, hamster and mouse neutrophil elastase, respectively[1].

体内活性: Sivelestat (ONO-5046, 0.021-2.1 mg/kg, intratracheally) suppresses lung hemorrhage in hamster (ID50 = 82 pg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which are induced by human neutrophil elastase[1]. Sivelestat (10 mg/kg, infusion via the tail vein) ameliorates lung injury after hemorrhagic shock in rats[2]. Sivelestat (15, 60 mg/kg, ip) prevents ischemia–reperfusion injury in the rat bladder[3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 225 mg/mL (425.7 mM)


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

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相关库: Drug Repurposing Compound Library | Approved Drug Library | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Viral Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途