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Sivelestat sodium tetrahydrate

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Catalog No. T20762Cas No. 201677-61-4
Alias Sivelestat Sodium Hydrate, Sivelestat Sodium, ONO-5046 sodium tetrahydrate, ONO5046 sodium tetrahydrate, ONO-5046, ONO5046, ONO 5046, Elaspol sodium tetrahydrate, Elaspol

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.

Sivelestat sodium tetrahydrate
Other Forms of Sivelestat sodium tetrahydrate:

Sivelestat sodium tetrahydrate

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Purity: 99.68%
Catalog No. T20762Alias Sivelestat Sodium Hydrate, Sivelestat Sodium, ONO-5046 sodium tetrahydrate, ONO5046 sodium tetrahydrate, ONO-5046, ONO5046, ONO 5046, Elaspol sodium tetrahydrate, ElaspolCas No. 201677-61-4
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.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$40In StockIn Stock
25 mg$77In StockIn Stock
50 mg$142In StockIn Stock
100 mg$208In StockIn Stock
200 mg$310-In Stock
1 mL x 10 mM (in DMSO)$44In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information

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Purity:99.68%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
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 hamsters (ID50 = 82 pg/kg) and increases skin capillary permeability in guinea pigs (ID50 = 9.6 mg/kg) via intravenous administration, both induced by human neutrophil elastase[1]. Additionally, Sivelestat (10 mg/kg, tail vein infusion) ameliorates lung injury after hemorrhagic shock in rats[2], and prevents ischemia-reperfusion injury in the rat bladder (15, 60 mg/kg, ip)[3].
SynonymsSivelestat Sodium Hydrate, Sivelestat Sodium, ONO-5046 sodium tetrahydrate, ONO5046 sodium tetrahydrate, ONO-5046, ONO5046, ONO 5046, Elaspol sodium tetrahydrate, Elaspol
Chemical Properties
Molecular Weight528.51
FormulaC20H29N2NaO11S
Cas No.201677-61-4
SmilesO.O.O.O.[NaH].CC(C)(C)C(=O)Oc1ccc(cc1)S(=O)(=O)Nc1ccccc1C(=O)NCC(O)=O
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 225 mg/mL (425.73 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.46 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8921 mL9.4606 mL18.9211 mL94.6056 mL
5 mM0.3784 mL1.8921 mL3.7842 mL18.9211 mL
10 mM0.1892 mL0.9461 mL1.8921 mL9.4606 mL
20 mM0.0946 mL0.4730 mL0.9461 mL4.7303 mL
50 mM0.0378 mL0.1892 mL0.3784 mL1.8921 mL
100 mM0.0189 mL0.0946 mL0.1892 mL0.9461 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

Sivelestat sodium TetrahydrateSivelestat sodiumSerineProteaseSerine ProteaseONO-5046 sodium TetrahydrateONO5046 sodium TetrahydrateONO-5046 sodiumONO5046 sodiumNeutrophil elastase (human)Elaspol sodium TetrahydrateElaspol sodium
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