Sivelestat

Catalog No.S8136 Batch:S813602

Technical Data

Formula

C₂₀H₂₂N₂O₇S

Molecular Weight

434.46

CAS No.

127373-66-4

Solubility (25°C)*

In vitro

DMSO

87 mg/mL (200.24 mM)

Ethanol

12 mg/mL (27.62 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

2% DMSO 1 40% PEG 300 2 5%Tween80 3 53%ddH2O

3.6mg/ml

Taking the 1 mL working solution as an example, add 20 μL of 180 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:^{^[2]}	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).
Animal Study:^{^[1]}	Animal Models Male Sprague-Dawley rats Dosages 50 or 100 mg/kg Administration i.p.

Cell Assay:^{^[2]}

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).

Animal Study:^{^[1]}

Animal Models
Male Sprague-Dawley rats
Dosages
50 or 100 mg/kg
Administration
i.p.

References

+ Expand

Selleck's Sivelestat has been cited by 14 publications

Cathepsin C inhibition reduces neutrophil serine protease activity and improves activated neutrophil-mediated disorders [ Nat Commun, 2024, 15(1):6519]	PubMed: 39174512
Neutrophil Extracellular Traps Mediate Acute Liver Failure in Regulation of miR-223/neutrophil Elastase Signaling in Mice [ Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00097-2]	PubMed: 35660025
Neutrophil extracellular traps mediate severe lung injury induced by influenza A virus H1N1 in mice coinfected with Staphylococcus aureus [ Microb Pathog, 2022, 166:105558]	PubMed: 35487479
Downregulation of Sepina3n Aggravated Blood-Brain Barrier Disruption after Traumatic Brain Injury by Activating Neutrophil Elastase in Mice [ Neuroscience, 2022, 503:45-57]	PubMed: 36089165
Chicken cathelicidin-2 promotes IL-1β secretion via the NLRP3 inflammasome pathway and serine proteases activity in LPS-primed murine neutrophils [ Dev Comp Immunol, 2022, 131:104377]	PubMed: 35189160
Gold nanoparticles synergize with bacterial lipopolysaccharide to enhance class A scavenger receptor dependent particle uptake in neutrophils and augment neutrophil extracellular traps formation [ Ecotoxicol Environ Saf, 2021, 211:111900]	PubMed: 33440266
Neutrophil extracellular DNA traps promote pancreatic cancer cells migration and invasion by activating EGFR/ERK pathway [ J Cell Mol Med, 2021, 10.1111/jcmm.16555]	PubMed: 33955688
Inhibition of Efferocytosis by Extracellular CIRP-Induced Neutrophil Extracellular Traps [ J Immunol, 2021, 206(4):797-806]	PubMed: 33380498
Cathepsin C promotes breast cancer lung metastasis by modulating neutrophil infiltration and neutrophil extracellular trap formation [ Cancer Cell, 2020, S1535-6108(20)30660-7]	PubMed: 33450198
Targeting High Mobility Group Box-1 (HMGB1) Promotes Cell Death in Myelodysplastic Syndrome [ Clin Cancer Res, 2019, 25(13):4155-4167]	PubMed: 30952643

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.