Sivelestat

製品コードS8136 バッチS813602

印刷

化学情報

Chemical Structure Synonyms ONO-5046, LY544349, EI546 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H22N2O7S
分子量 434.46 CAS No. 127373-66-4
Solubility (25°C)* 体外 DMSO 87 mg/mL (200.24 mM)
Ethanol 12 mg/mL (27.62 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
2% DMSO 40% PEG 300 5%Tween80 53%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 3.600mg/ml (8.29mM) 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 TMK-1 gastric carcinoma cells
濃度 0.1–1000 µg/mL
反応時間 24, 48 or 72 h
実験の流れ

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).
動物実験 動物モデル Male Sprague-Dawley rats
投薬量 50 or 100 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/27430552/
  • http://onlinelibrary.wiley.com/doi/10.1111/j.1349-7006.2006.00278.x/pdf
  • https://pubmed.ncbi.nlm.nih.gov/19169649/
  • https://pubmed.ncbi.nlm.nih.gov/21221803/
  • https://pubmed.ncbi.nlm.nih.gov/27256506/
  • https://pubmed.ncbi.nlm.nih.gov/22148910/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Neutrophil extracellular traps exacerbate inflammatory arthritis by inhibiting γδ Treg cell differentiation via the AIM2 inflammasome [ Redox Biol, 2025, 87:103881] PubMed: 41046783
Neutrophil extracellular traps impede cancer metastatic seeding via protease-activated receptor 2-mediated downregulation of phagocytic checkpoint CD24 [ J Immunother Cancer, 2025, 13(2)e010813] PubMed: 40010762
Paeonol inhibits NETs-mediated foam cell inflammation through the CitH3/NLRP3/caspase-1 signaling pathway in atherosclerosis [ Int Immunopharmacol, 2025, 151:114340] PubMed: 40020464
Research on the process and molecular mechanism of inhibiting serous ovarian cancer by PRTN3 and its inhibitor Sivelestat [ J Ovarian Res, 2025, 18(1):211] PubMed: 41023684
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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