产品
编 号：F248982
分子式：C20H29N2NaO11S
分子量：528.51
分子式：C20H29N2NaO11S
分子量：528.51
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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50mg
询价
询价
100mg
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结构图
CAS No: 201677-61-4
产品详情
生物活性：
Sivelestat (EI546) 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.
体内研究：
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.Animal Model:Male Golden hamsters, weighing 90 to 110 g.
Dosage:0.021-2.1 mg/kg.
Administration:Intratracheally five min before HNE injection.
Result:Significantly and dosedependently suppressed the lung hemorrhage.
Animal Model:Male Sprague-Dawley rats weighing 350-400 g.
Dosage:10 mg/kg.
Administration:Continuous infusion via the tail vein at 10 mg/kg/h for 60 min during the resuscitation phase.
Result:Greatly suppressed lung injury, as revealed by the reduced histological damage.Significantly ameliorated HSR-induced lung injury.Markedly decreased the levels of TNF-α and iNOS gene.
Animal Model:Male Sprague Dawley rats, 8 weeks old and weighing 250-320 g.
Dosage:15 mg/kg or 60 mg/kg.
Administration:IP.
Result:Decreased the blood flow in the bladder during reperfusion phase compared to the IR group.
体外研究：
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.
Sivelestat (EI546) 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.
体内研究：
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.Animal Model:Male Golden hamsters, weighing 90 to 110 g.
Dosage:0.021-2.1 mg/kg.
Administration:Intratracheally five min before HNE injection.
Result:Significantly and dosedependently suppressed the lung hemorrhage.
Animal Model:Male Sprague-Dawley rats weighing 350-400 g.
Dosage:10 mg/kg.
Administration:Continuous infusion via the tail vein at 10 mg/kg/h for 60 min during the resuscitation phase.
Result:Greatly suppressed lung injury, as revealed by the reduced histological damage.Significantly ameliorated HSR-induced lung injury.Markedly decreased the levels of TNF-α and iNOS gene.
Animal Model:Male Sprague Dawley rats, 8 weeks old and weighing 250-320 g.
Dosage:15 mg/kg or 60 mg/kg.
Administration:IP.
Result:Decreased the blood flow in the bladder during reperfusion phase compared to the IR group.
体外研究：
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.
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