受注:045-509-1970 |
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Synonyms | ONO-5046, LY544349, EI546 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C20H22N2O7S |
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分子量 | 434.46 | CAS No. | 127373-66-4 | ||||
Solubility (25°C)* | 体外 | DMSO | 86 mg/mL (197.94 mM) | ||||
Ethanol | 8 mg/mL (18.41 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
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. |
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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. |
細胞アッセイ | 細胞株 | TMK-1 gastric carcinoma cells |
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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). |
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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. |
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。