| Name | Sivelestat |
| Description | Sivelestat (ONO5046) is a potent and selective inhibitor of neutrophil elastase with IC50 of 44 nM. |
| Cell Research | TMK-1 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. |
| Animal Research | Animal Models: Male Sprague-Dawley rats. Formulation: Saline. Dosages: 50 or 100 mg/kg. Administration: i.p. |
| In vitro | Sivelestat suppresses iNOS gene expression in proinflammatory cytokine-stimulated hepatocytes. Sivelestat reduces the levels of inflammatory mediators by inhibiting NF-kB. It suppresses the growth of gastric cancer cells by inhibiting the release of TGF-α stimulated by NE. |
| In vivo | Administration of sivelestat attenuates pulmonary fibrosis after acute lung injury in mice. Sivelestat could attenuate sepsis-related kidney injury in rats. It blocks GAPDH/Siah1 which is a novel signaling pathway during the progression of spinal cord injury. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 80 mg/mL (184.14 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.6 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 45 mg/mL (103.58 mM), Sonication is recommended.
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| Keywords | Sivelestat | SerineProtease | Serine Protease | SARS-CoV | SARSCoV | SARS coronavirus | reperfusion | ONO-5046 | ONO 5046 | neutrophil elastase | LY-544349 | LY 544349 | lung | ischemia | injury | Inhibitor | inhibit | Elastase | EI-546 | EI 546 | Acute |
| Inhibitors Related | Remdesivir | Silymarin | Molnupiravir | AEBSF hydrochloride | Hydroxychloroquine | Ritonavir | Imidazole | Chloroquine phosphate | Subtilisin | α-Cyclodextrin | Dexamethasone | Ac-Ala-OH |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
