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Sivelestat

SKU: orb1300286

Description

Sivelestat (ONO5046) is a highly selective neutrophil elastase inhibitor with an IC50 of 44 nM. It is widely used in research on acute lung injury (ALI), acute respiratory distress syndrome (ARDS), and other inflammatory conditions, with applications in both in vitro and in vivo experimental models.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Images & Validation

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Sivelestat

Key Properties

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CAS Number127373-66-4
MW434.46
Purity99.54% (May vary between batches)
FormulaC20H22N2O7S
SMILESCC(C)(C)C(=O)Oc1ccc(cc1)S(=O)(=O)Nc1ccccc1C(=O)NCC(O)=O
TargetSerine Protease,SARS-CoV
SolubilityDMSO:45 mg/mL (103.58 mM);Ethanol:80 mg/mL (184.14 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.6 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50
Neutrophil elastase:44 nM.
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.
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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.
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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.
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Animal Research
Animal Models: Male Sprague-Dawley rats. Formulation: Saline. Dosages: 50 or 100 mg/kg. Administration: i.p.

Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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reperfusion, SARS-CoV, SARS coronavirus, SARSCoV, Serine Protease, SerineProtease, Sivelestat, ONO 5046, ONO5046, ONO-5046, neutrophil elastase, LY 544349, LY544349, LY-544349, lung, ischemia, inhibit, Inhibitor, injury, Elastase, EI 546, EI546, EI-546, Acute

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Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID
107706 ↗

Key Properties

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No computed properties available.

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Sivelestat (orb1300286)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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2 mg
$ 70.00
5 mg
$ 80.00
1 ml x 10 mM (in DMSO)
$ 110.00
10 mg
$ 110.00
25 mg
$ 150.00
50 mg
$ 250.00
100 mg
$ 360.00
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