产品
编 号：F107096
分子式：C20H22N2O7S
分子量：434.46
分子式：C20H22N2O7S
分子量：434.46
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
175
In-stock
5mg
350
In-stock
10mg
560
In-stock
50mg
1920
In-stock
结构图
CAS No: 127373-66-4
产品详情
生物活性：
Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) 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，气管内) 通过气管内给药抑制仓鼠肺出血 (ID50=82 pg/kg) 并增加豚鼠皮肤毛细血管通透性 (ID50=9.6 mg/kg) 通过静脉给药，均由人中性粒细胞弹性蛋白酶诱导。Sivelestat (10 mg/kg，输注通过尾静脉) 改善大鼠失血性休克后的肺损伤。Sivelestat (15、60 mg/kg，腹腔注射) 可预防大鼠膀胱的缺血再灌注损伤。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) 不抑制胰蛋白酶、凝血酶、纤溶酶、血浆激肽释放酶、胰腺激肽释放酶、胰凝乳蛋白酶和组织蛋白酶 G，即使浓度为 100 μM。 Sivelestat (ONO-5046) 对人、兔、大鼠、仓鼠和小鼠中性粒细胞弹性蛋白酶的 IC50 值分别为 44 nM、36 nM、19 nM、37 nM 和 49 nM。
Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) 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，气管内) 通过气管内给药抑制仓鼠肺出血 (ID50=82 pg/kg) 并增加豚鼠皮肤毛细血管通透性 (ID50=9.6 mg/kg) 通过静脉给药，均由人中性粒细胞弹性蛋白酶诱导。Sivelestat (10 mg/kg，输注通过尾静脉) 改善大鼠失血性休克后的肺损伤。Sivelestat (15、60 mg/kg，腹腔注射) 可预防大鼠膀胱的缺血再灌注损伤。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) 不抑制胰蛋白酶、凝血酶、纤溶酶、血浆激肽释放酶、胰腺激肽释放酶、胰凝乳蛋白酶和组织蛋白酶 G，即使浓度为 100 μM。 Sivelestat (ONO-5046) 对人、兔、大鼠、仓鼠和小鼠中性粒细胞弹性蛋白酶的 IC50 值分别为 44 nM、36 nM、19 nM、37 nM 和 49 nM。
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