Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H21N2O7S.Na.4H2O |
| Molecular Weight | 528.506 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.O.O.O.[Na+].CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=C(C=CC=C2)C(=O)NCC([O-])=O
InChI
InChIKey=PLHREJBSQUSUCW-UHFFFAOYSA-M
InChI=1S/C20H22N2O7S.Na.4H2O/c1-20(2,3)19(26)29-13-8-10-14(11-9-13)30(27,28)22-16-7-5-4-6-15(16)18(25)21-12-17(23)24;;;;;/h4-11,22H,12H2,1-3H3,(H,21,25)(H,23,24);;4*1H2/q;+1;;;;/p-1
Sivelestat is a neutrophil elastase inhibitor approved in Japan and the Republic of Korea for acute lung injury, including acute respiratory distress syndrome in patients with systemic inflammatory response syndrome. Sivelestat is marketed as Elaspol in Japan. Sivelestat competitively inhibited human neutrophil elastase (IC50 = 0.044 uM, Ki = 0.2 uM). It also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Effects of sivelestat sodium hydrate on the reduction of radiation pneumonitis. | 2007 Dec |
|
| A neutrophil elastase inhibitor, sivelestat, improved respiratory and cardiac function in pediatric cardiovascular surgery with cardiopulmonary bypass. | 2008 |
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| Neutrophil Proteases Activate Eosinophil Function in vitro. | 2008 |
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| Severe Legionnaires' disease successfully treated using a combination of fluoroquinolone, erythromycin, corticosteroid, and sivelestat. | 2008 |
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| A neutrophil elastase inhibitor, sivelestat, reduces lung injury following endotoxin-induced shock in rats by inhibiting HMGB1. | 2008 Aug |
|
| Inhibition of neutrophil elastase reduces lung injury and bacterial count in hamsters. | 2008 Dec |
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| Beneficial effect of neutrophil elastase inhibitor on anti-Thy1.1 nephritis in rats. | 2008 Feb |
|
| Continuous infusion of sivelestat sodium hydrate prevents lipopolysaccharide-induced intestinal paralysis and hypotension in conscious guinea-pigs. | 2008 Jul |
|
| [Effect of sivelestat sodium on acute lung injury after acute aortic dissection]. | 2008 Jun |
|
| Sivelestat and its role in tissue reperfusion injury. | 2008 Jun |
|
| Neutrophil elastase activity in acute lung injury and respiratory distress syndrome. | 2008 Jun |
|
| Protective effect of Sivelestat in a porcine hepatectomy model prepared using an intermittent Pringle method. | 2008 Jun 10 |
|
| [A case of lung adenocarcinoma effectively treated with sivelestat and corcicosteroid for drug-induced lung disease due to gefitinib]. | 2008 Mar |
|
| Sivelestat relaxes porcine coronary artery via inhibition of Ca2+ sensitization induced by a receptor agonist. | 2008 May |
|
| Usefulness of a selective neutrophil elastase inhibitor (sivelestat) in septic ARDS patients after gastrointestinal surgery. | 2008 May-Jun |
|
| [Efficacy of sivelestat for acute lung injury due to severe bacterial pneumonia with systemic inflammatory response syndrome]. | 2008 Oct |
|
| [Case of transfusion-related acute lung injury associated with severe intraoperative hypoxemia]. | 2008 Oct |
|
| Sivelestat attenuates postoperative pulmonary dysfunction after total arch replacement under deep hypothermia. | 2008 Oct |
|
| Protective effect of sivelestat sodium (Eraspol) on postoperative lung dysfunction in patients with type A acute aortic dissection: a pilot study. | 2008 Oct |
|
| The effect of sivelestat sodium on post-cardiopulmonary bypass acute lung injury in a neonatal piglet model. | 2008 Oct |
|
| Role of neutrophil elastase in development of pulmonary vascular injury and septic shock in rats. | 2008 Oct |
|
| Sivelestat treatment for acute respiratory distress syndrome in an infant. | 2009 |
|
| Resuscitation of haemorrhagic shock with normal saline vs. lactated Ringer's: effects on oxygenation, extravascular lung water and haemodynamics. | 2009 |
|
| Plasma neutrophil elastase and elafin imbalance is associated with acute respiratory distress syndrome (ARDS) development. | 2009 |
|
| Neutrophil elastase inhibitor (sivelestat) reduces the levels of inflammatory mediators by inhibiting NF-kB. | 2009 Apr |
|
| Prevention of leukocyte activation by the neutrophil elastase inhibitor, sivelestat, in the hepatic microcirculation after ischemia-reperfusion. | 2009 Aug |
|
| A pilot randomized study of the neutrophil elastase inhibitor, Sivelestat, in patients undergoing cardiac surgery. | 2009 Aug |
|
| Effects of elastase inhibitor on the epithelial cell apoptosis in bleomycin-induced pulmonary fibrosis. | 2009 Dec |
|
| Sivelestat reduces myocardial ischemia and reperfusion injury in rat hearts even when administered after onset of myocardial ischemia. | 2009 Jun |
|
| Neutrophil elastase activity compensates for a genetic lack of matrix metalloproteinase-9 (MMP-9) in leukocyte infiltration in a model of experimental peritonitis. | 2009 Mar |
|
| Effect of neutrophil elastase inhibitor (sivelestat sodium) in the treatment of acute lung injury (ALI) and acute respiratory distress syndrome (ARDS): a systematic review and meta-analysis. | 2010 |
|
| Mechanical strength and viscoelastic response of the periodontal ligament in relation to structure. | 2010 |
|
| DAMPening inflammation by modulating TLR signalling. | 2010 |
|
| Platelet adhesion in the sinusoid caused hepatic injury by neutrophils after hepatic ischemia reperfusion. | 2010 |
|
| Efficacy of neutrophil elastase inhibitor on type A acute aortic dissection. | 2010 Apr |
|
| The impact of oxidative stress levels on the clinical effectiveness of sivelestat in treating acute lung injury: an electron spin resonance study. | 2010 Apr |
|
| Extracorporeal immune therapy with immobilized agonistic anti-Fas antibodies leads to transient reduction of circulating neutrophil numbers and limits tissue damage after hemorrhagic shock/resuscitation in a porcine model. | 2010 Apr 20 |
|
| Postischemic infusion of sivelestat sodium hydrate, a selective neutrophil elastase inhibitor, protects against myocardial stunning in swine. | 2010 Aug |
|
| Suppressive effects of sivelestat on interleukin 8 and TNF-α production from LPS-stimulated granulocytes in whole blood culture. | 2010 Dec |
|
| Neutrophil elastase inhibitor restores gut ischemia reperfusion-induced impairment of gut immunity with reduced plasma interleukin-6 concentrations in mice. | 2010 Dec |
|
| Sivelestat (selective neutrophil elastase inhibitor) improves the mortality rate of sepsis associated with both acute respiratory distress syndrome and disseminated intravascular coagulation patients. | 2010 Jan |
|
| Neutrophil elastase inhibitor prevents ischemic brain damage via reduction of vasogenic edema. | 2010 Jul |
|
| Neutrophil elastase contributes to the development of ischemia/reperfusion-induced liver injury by decreasing the production of insulin-like growth factor-I in rats. | 2010 Jun |
|
| Effect of a neutrophil elastase inhibitor on acute lung injury after cardiopulmonary bypass. | 2010 Jun |
|
| Neutrophil elastase inhibitor improves survival of rats with clinically relevant sepsis. | 2010 May |
|
| The protective function of neutrophil elastase inhibitor in liver ischemia/reperfusion injury. | 2010 May 15 |
|
| In vivo efficacy of sivelestat in combination with pazufloxacin against Legionella pneumonia. | 2010 Oct |
|
| Prognostic impact of clinical course-specific mRNA expression profiles in the serum of perioperative patients with esophageal cancer in the ICU: a case control study. | 2010 Oct 22 |
|
| Effect of a selective neutrophil elastase inhibitor on early recovery from body water imbalance after transthoracic esophagectomy. | 2010 Sep |
|
| Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase. | 2011 Aug 1 |
Patents
Sample Use Guides
0.2 mg/kg/hr continuous i.v. infusion - up to 14 days
Route of Administration:
Intravenous
Addition of 10 or 100 ug/ml sivelestat significantly (P < 0.05) inhibited the production of TNF-α from granulocytes induced by 10 ng/ml LPS. Granulocytic production of IL-8 induced by 1 ng/ml LPS was significantly (P < 0.05) inhibited by treatment with 1 ug/ml sivelestat, and upregulation of IL-8 by 10 ng/ml LPS was also significantly (P < 0.05) suppressed by 1 and 10 ug/ml sivelestat.
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NCI_THESAURUS |
C783
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158792
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m9966
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OO-54
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300000032191
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CHEMBL76688
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SUB22092
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C76910
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DTXSID0046727
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ACTIVE MOIETY
SUBSTANCE RECORD
