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Sivelestat

Catalog No. T6986   CAS 127373-66-4
Synonyms: ONO5046, EI546, LY544349

Sivelestat (ONO5046) is a potent and selective inhibitor of neutrophil elastase with IC50 of 44 nM.

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Sivelestat Chemical Structure
Sivelestat, CAS 127373-66-4
Pack Size Availability Price/USD Quantity
5 mg In stock $ 42.00
10 mg In stock $ 61.00
25 mg In stock $ 110.00
50 mg In stock $ 210.00
100 mg In stock $ 315.00
200 mg In stock $ 523.00
500 mg In stock $ 837.00
1 mL * 10 mM (in DMSO) In stock $ 68.00
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Purity: 99.52%
Purity: 99.22%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Sivelestat (ONO5046) is a potent and selective inhibitor of neutrophil elastase with IC50 of 44 nM.
Targets&IC50 neutrophil elastase:44 nM.
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.
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.
Synonyms ONO5046, EI546, LY544349
Molecular Weight 434.46
Formula C20H22N2O7S
CAS No. 127373-66-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 80 mg/mL (184.1 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 80 mg/mL (184.1 mM)

TargetMolReferences and Literature

1. Li G, et al. Int J Mol Med. 2016, 38(3):767-75. 2. Wada Y, et al. Cancer Science. 2006, 97(10):1037-1043. 3. Hagiwara S, et al. Inflamm Res. 2009, 58(4):198-203. 4. Araki Y, et al. Dig Dis Sci. 2011, 56(6):1672-81. 5. Huo J, et al. Neuroscience. 2016, 330:171-180.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Bioactive Compounds Library Max Inhibitor Library Anti-Aging Compound Library Anti-Viral Compound Library FDA-Approved & Pharmacopeia Drug Library Bioactive Compound Library

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Keywords

Sivelestat 127373-66-4 Microbiology/Virology Others Proteases/Proteasome SARS-CoV Serine Protease ONO5046 Inhibitor ischemia LY-544349 inhibit LY 544349 Acute EI546 reperfusion EI-546 EI 546 SARS coronavirus injury ONO 5046 Elastase lung ONO-5046 LY544349 inhibitor

 

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