Sivelestat (ONO-5046)

For research use only.

Catalog No.S8136 Synonyms: ONO5046, LY544349, EI546

3 publications

Sivelestat (ONO-5046) Chemical Structure

Molecular Weight(MW): 434.46

Sivelestat is a potent and selective inhibitor of neutrophil elastase with IC50 of 44nM. It almost shows no activity at a range of other proteases.

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Choose Selective Serine Protease Inhibitors

Biological Activity

Description Sivelestat is a potent and selective inhibitor of neutrophil elastase with IC50 of 44nM. It almost shows no activity at a range of other proteases.
Targets
neutrophil elastase [1]
In vitro

sivelestat reduces the levels of inflammatory mediators by inhibiting NF-kB[3]. It suppresses the growth of gastric cancer cells by inhibiting the release of TGF-α stimulated by NE[2]; Sivelestat suppresses iNOS gene expression in proinflammatory cytokine-stimulated hepatocytes[4].

In vivo sivelestat could attenuate sepsis-related kidney injury in rats[1]. It blocks GAPDH/Siah1 which is a novel signaling pathway during the progression of spinal cord injury[5]. Administration of sivelestat attenuates pulmonary fibrosis after acute lung injury in mice.

Protocol

Cell Research:

[2]

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  • Cell lines: TMK-1 gastric carcinoma cells
  • Concentrations: 0.1–1000 µg/mL
  • Incubation Time: 24, 48 or 72 h
  • Method:

    Gastric carcinoma cells are seeded into 96-well culture plates (5 × 103 cells/well) in RPMI containing 7% FBS, 2.0 mM L-glutamine, and 1% nonessential amino acids. Following 24-h incubation in RPMI-1640 medium with 5% FBS, the cells are incubated for 24, 48 or 72 h at 37°C in a humidified atmosphere of 5% CO2 with varied concentrations (0.1–1.0 µg/mL) of NE, or with varied concentrations (0.1–1000 µg/mL) of sivelestat or with concentrations (10 and 100 ng/mL) of anti-TGF-α antibody in the presence of 1 µg/mL NE. After incubation, 10 µL of MTT solution (5 mg/mL) is added to each well and the plates are then incubated for 3 h at 37°C. The growth medium is then replaced with 150 µL of dimethyl sulfoxide (Wako) per well and the absorbance at 540 nm is measured using a Titertek Multiscan (Titertek, Huntsville, AL).


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Male Sprague-Dawley rats
  • Dosages: 50 or 100 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (197.94 mM)
Ethanol 86 mg/mL (197.94 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
23mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 434.46
Formula

C20H22N2O7S

CAS No. 127373-66-4
Storage powder
in solvent
Synonyms ONO5046, LY544349, EI546
Smiles CC(C)(C)C(=O)OC1=CC=C(C=C1)[S](=O)(=O)NC2=CC=CC=C2C(=O)NCC(O)=O

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID