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Sivelestat sodium tetrahydrate

CAS No. : 201677-61-4

MCE 站：Sivelestat sodium tetrahydrate

产品活性：Sivelestat (EI546) 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， K_i 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。

研究领域：Metabolic Enzyme/Protease  |  Anti-infection

作用靶点：Elastase  |  SARS-CoV

In Vitro: Sivelestat (ONO-5046) does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM.
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.

In Vivo: 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.
Sivelestat (10 mg/kg, infusion via the tail vein) ameliorates lung injury after hemorrhagic shock in rats.
Sivelestat (15, 60 mg/kg, ip) prevents ischemia–reperfusion injury in the rat bladder.

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