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Sivelestat sodium tetrahydrate

Catalog No. T20762   CAS 201677-61-4
Synonyms: ONO-5046 sodium tetrahydrate, Elaspol, ONO 5046, ONO5046 sodium tetrahydrate, Elaspol sodium tetrahydrate, ONO-5046, Sivelestat Sodium, Sivelestat Sodium Hydrate, ONO5046

Sivelestat sodium tetrahydrate (ONO5046 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.

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Sivelestat sodium tetrahydrate Chemical Structure
Sivelestat sodium tetrahydrate, CAS 201677-61-4
Pack Size Availability Price/USD Quantity
5 mg In stock $ 42.00
10 mg In stock $ 67.00
25 mg In stock $ 129.00
50 mg In stock $ 237.00
100 mg In stock $ 347.00
200 mg In stock $ 516.00
1 mL * 10 mM (in DMSO) In stock $ 74.00
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Purity: 99.64%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Sivelestat sodium tetrahydrate (ONO5046 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.
In vitro Sivelestat (ONO-5046) is not an inhibitor of trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin, or cathepsin G, even at concentrations up to 100 μM[1]. However, it effectively inhibits neutrophil elastase across various species, demonstrating IC50 values of 44 nM (human), 36 nM (rabbit), 19 nM (rat), 37 nM (hamster), and 49 nM (mouse), showcasing its specificity and potential for therapeutic applications[1].
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[1]. Sivelestat (10 mg/kg, infusion via the tail vein) ameliorates lung injury after hemorrhagic shock in rats[2]. Sivelestat (15, 60 mg/kg, ip) prevents ischemia–reperfusion injury in the rat bladder[3].
Synonyms ONO-5046 sodium tetrahydrate, Elaspol, ONO 5046, ONO5046 sodium tetrahydrate, Elaspol sodium tetrahydrate, ONO-5046, Sivelestat Sodium, Sivelestat Sodium Hydrate, ONO5046
Molecular Weight 528.51
Formula C20H29N2NaO11S
CAS No. 201677-61-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 225 mg/mL (425.7 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Kawabata K, et al. ONO-5046, a novel inhibitor of human neutrophil elastase. Biochem Biophys Res Commun. 1991 Jun 14;177(2):814-20. 2. Yuichiro Toda, et al. A neutrophil elastase inhibitor, sivelestat, ameliorates lung injury after hemorrhagic shock in rats. Int J Mol Med. 2007 Feb;19(2):237-43. 3. Tomoharu Kono, et al. Neutrophil elastase inhibitor, sivelestat sodium hydrate prevents ischemia-reperfusion injury in the rat bladder. Mol Cell Biochem. 2008 Apr;311(1-2):87-92. 4. Adeleh Sahebnasagh, et al. Neutrophil elastase inhibitor (sivelestat) may be a promising therapeutic option for management of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19. J Clin Pharm Ther. 2

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Inhibitor Library Anti-Viral Compound Library Approved Drug Library Bioactive Compounds Library Max FDA-Approved & Pharmacopeia Drug Library Bioactive Compound Library

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Keywords

Sivelestat sodium tetrahydrate 201677-61-4 Proteases/Proteasome Serine Protease ONO-5046 sodium tetrahydrate Elaspol ONO-5046 sodium Tetrahydrate ONO 5046 ONO5046 sodium tetrahydrate Elaspol sodium tetrahydrate Elaspol sodium ONO-5046 ONO5046 sodium Sivelestat Sodium Sivelestat sodium ONO5046 sodium Tetrahydrate ONO-5046 sodium Elaspol sodium Tetrahydrate Sivelestat sodium Tetrahydrate Sivelestat Sodium Hydrate ONO5046 inhibitor inhibit

 

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