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Submit ReviewSivelestat sodium salt is a selective leukocyte elastase inhibitor (IC50 = 44 nM) that displays no activity at a range of other proteases. Inhibits NF-κB activation and LTB4-induced neutrophil transmigration in vitro. Significantly attenuates ischemia-induced spinal cord injury, decreases serum cytokine levels and reduces acute inflammatory lung injury in vivo.
Sivelestat sodium salt is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 456.44 |
Formula | C20H21N2NaO7S |
Storage | Desiccate at RT |
Purity | ≥98% (HPLC) |
CAS Number | 150374-95-1 |
PubChem ID | 23664980 |
InChI Key | ZAIFANJZUGNYCK-UHFFFAOYSA-M |
Smiles | [Na+].CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC1=CC=CC=C1C(=O)NCC([O-])=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 22.82 | 50 |
The following data is based on the product molecular weight 456.44. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4.38 mL | 21.91 mL | 43.82 mL |
2.5 mM | 0.88 mL | 4.38 mL | 8.76 mL |
5 mM | 0.44 mL | 2.19 mL | 4.38 mL |
25 mM | 0.09 mL | 0.44 mL | 0.88 mL |
References are publications that support the biological activity of the product.
Kawabata et al (1991) ONO-5046, a novel inhibitor of human neutrophil elastase. Biochem.Biophys.Res.Commun. 177 814 PMID: 2049103
Young et al (2007) Role of neutrophil elastase in LTB4-induced neutrophil transmigration in vivo assessed with a specific inhibitor and neutrophil elastase deficient mice. Br.J.Pharmacol. 151 628 PMID: 17471175
Hagiwara et al (2009) Neutrophil elastase inhibitor (sivelestat) reduces the levels of inflammatory mediators by inhibiting NF-κB. Inflamm.Res. 58 198 PMID: 19169649
Iwamoto et al (2009) Protective effect of sivelestat sodium hydrate (ONO-5046) on ischemic spinal cord injury. Interact.Cardiovasc.Thorac.Surg. 8 606 PMID: 19289399
If you know of a relevant reference for Sivelestat sodium salt, please let us know.
Keywords: Sivelestat sodium salt, Sivelestat sodium salt supplier, Selective, leukocyte, elastase, inhibitors, inhibits, Human, Neutrophil, Proteinases, Proteases, ONO5046, ONO-5046, Elastase, 3535, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Sivelestat sodium salt include:
Saadoun et al (2012) Neutrophil protease inhibition reduces neuromyelitis optica-immunoglobulin G-induced damage in mouse brain. J Neurosci 71 323 PMID: 22374891
Marcin et al (2022) Camostat Does Not Inhibit the Proteolytic Activity of Neutrophil Serine Proteases. Pharmaceuticals (Basel) 15 PMID: 35631327
Berg et al (2019) Proteolytic and Opportunistic Breaching of the Basement Membrane Zone by Immune Cells during Tumor Initiation. Cell Rep 27 2837 PMID: 31167131
Javier et al (2020) Neutrophil elastase from myeloid cells promotes TSC2-null tumor growth. Endocr Relat Cancer 27 261-274 PMID: 32045362
Albrengues et al (2018) Neutrophil extracellular traps produced during inflammation awaken dormant cancer cells in mice. Science 361 PMID: 30262472
Masood et al (2015) Neutrophil elastase-induced elastin degradation mediates macrophage influx and lung injury in 60% O2-exposed neonatal rats. Am J Physiol Lung Cell Mol Physiol 309 L53 PMID: 26136527
Do you know of a great paper that uses Sivelestat sodium salt from Tocris? Please let us know.
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