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）
Clear solution
2% DMSO 40% PEG 300 5%Tween80 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.

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.

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 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
Overexpression of MTA1 inhibits the metastatic ability of ZR-75-30 cells in vitro by promoting MTA2 degradation [ Cell Commun Signal, 2019, 17(1):4] PubMed: 30642362

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。