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Sivelestat sodium (EI 546 sodium) is a highly efficient inhibitor of human neutrophil elastase, improving sepsis-induced myocardial dysfunction by activating the PI3K/AKT/mTOR signaling pathway. It can be used in acute lung injury/acute respiratory distress syndrome research.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $30 | In Stock | |
1 mL x 10 mM (in DMSO) | $77 | 5 days |
Description | Sivelestat sodium (EI 546 sodium) is a highly efficient inhibitor of human neutrophil elastase, improving sepsis-induced myocardial dysfunction by activating the PI3K/AKT/mTOR signaling pathway. It can be used in acute lung injury/acute respiratory distress syndrome research. |
Targets&IC50 | Neutrophil elastase (hamster):37 nM, Neutrophil elastase (rat):19 nM, Neutrophil elastase (rabbit):36 nM, Neutrophil elastase (human):200 nM (Ki), Neutrophil elastase (mouse):49 nM, Neutrophil elastase (human):44 nM |
In vitro | Sivelestat sodium, a competitive inhibitor of human neutrophil elastase, has a Ki value of 200 nM, and does not inhibit trypsin, thrombin, fibrinolytic enzymes, plasma kallikrein-releasing enzyme, pancreatic kallikrein-releasing enzyme, chytolysin, or histone G, even at concentrations up to 100 μM. The IC50 values of Sivelestat sodium on neutrophil elastase in different species are 44 nM in humans, 36 nM in rabbits, 19 nM in rats, 37 nM in hamsters, and 49 nM in mice.[1] |
In vivo | By intratracheal administration (0.021-2.1 mg/kg), Sivelestat sodium was able to effectively inhibit hamster lung hemorrhage induced by human neutrophil elastase (ID50 = 82 pg/kg), as well as the increase in guinea pig skin capillary permeability caused by i.v. administration (ID50 = 9.6 mg/kg). [1] Sivelestat sodium (10 mg/kg via tail vein infusion) ameliorated lung injury due to hemorrhagic shock in rats. [2] Sivelestat sodium was able to prevent ischemia-reperfusion injury in the bladder of rats by intraperitoneal injection (15 mg/kg and 60 mg/kg). [3] |
Alias | ONO5046 sodium, ONO 5046 sodium, LY-544349 sodium, LY544349 sodium, EI546 sodium, EI 546 sodium |
Molecular Weight | 456.45 |
Formula | C20H21N2NaO7S |
Cas No. | 150374-95-1 |
Smiles | O=C(CNC(C1=C(NS(=O)(C2=CC=C(C=C2)OC(C(C)(C)C)=O)=O)C=CC=C1)=O)[O-].[Na+] |
Relative Density. | 1.31g/cm3 |
Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80.00 mg/mL (175.27 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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