| 名称 | Sivelestat |
| 描述 | Sivelestat (ONO5046) is a potent and selective inhibitor of neutrophil elastase with IC50 of 44 nM. |
| 细胞实验 | 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. |
| 动物实验 | Animal Models: Male Sprague-Dawley rats. Formulation: Saline. Dosages: 50 or 100 mg/kg. Administration: i.p. |
| 体外活性 | 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. |
| 体内活性 | 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. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : 80 mg/mL (184.1 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 45 mg/mL (103.58 mM)
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| 关键字 | Inhibitor | ischemia | LY-544349 | inhibit | LY 544349 | Acute | reperfusion | EI-546 | EI 546 | Sivelestat | SARS coronavirus | injury | ONO 5046 | Elastase | lung | ONO-5046 | SARS-CoV |
| 相关产品 | Nirmatrelvir | EIDD-1931 | Remdesivir | Silymarin | AEBSF hydrochloride | Umifenovir hydrochloride | Hydroxychloroquine | Ritonavir | Chloroquine phosphate | Favipiravir |
| 相关库 | FDA上市及药典收录分子库 | 经典已知活性库 | 抗癌临床化合物库 | 抗病毒库 | 药物功能重定位化合物库 | 抑制剂库 | 抗癌上市药物库 | 已知活性化合物库 | 抗癌药物库 | 抗癌活性化合物库 |
United States
