Sivelestat sodium is a competitive inhibitor of human neutrophil elastase (IC50 = 44 nM; Ki=200 nM); also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse.
Sivelestat (EI546) sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM.This compound is under investigation for its potential use in the treatment of acute lung injury/acute respiratory distress syndrome (ALI/ARDS) or disseminated intravascular coagulation (DIC), particularly in the context of COVID-19[1].[2].[3].[4].
Sivelestat Sodium Tetrahydrate/西维来司钠四水合物 动物研究
Animal study
When administered intratracheally at dosages ranging from 0.021 to 2.1 mg/kg, Sivelestat significantly suppresses lung hemorrhage in hamsters (ID50 = 82 pg/kg) and reduces the increase of skin capillary permeability in guinea pigs (ID50 = 9.6 mg/kg), both of which are induced by human neutrophil elastase[1].Additionally, the compound, when infused via the tail vein at a dose of 10 mg/kg, has been shown to ameliorate lung injury following hemorrhagic shock in rats[2]. Furthermore, at doses of 15 and 60 mg/kg administered intraperitoneally, Sivelestat effectively prevents ischemia-reperfusion injury in the rat bladder[3].
搜索
