Sivelestat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、特异性和竞争性的人中性粒细胞弹性蛋白酶抑制剂，IC50 为 44 nM。

A potent, specific and competitive inhibitor of human neutrophil elastase with IC50 of 44 nM; also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse, do not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G (>10 uM); attenuates LPS-induced acute lung inflammation in the hamster.Other Indication Approved(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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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.

EI-546 | LY-544349 | ONO-5046

Metabolic Enzyme/Protease

Elastase

neutrophilelastase

Other Indications

Other Disease

127373-66-4

434.4629

C20H22N2O7S

>98% (HPLC)

10 mM in DMSO

CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC=CC=C2C(=O)NCC(=O)O

Propanoic acid, 2,2-dimethyl-, 4-[[[2-[[(carboxymethyl)amino]carbonyl]phenyl]amino]sulfonyl]phenyl ester

(-20℃)

With Ice Pack

≥ 2 years