Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Sivelestat (ONO5046) 是一种选择性的中性粒细胞弹性蛋白酶抑制剂,其 IC50值为 44 nM,Ki 值为 200 nM。它有潜力研究 COVID-19 的急性肺损伤、急性呼吸窘迫综合征或弥散性血管内凝血。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 158 | 现货 | ||
5 mg | ¥ 331 | 现货 | ||
10 mg | ¥ 578 | 现货 | ||
25 mg | ¥ 1,070 | 现货 | ||
50 mg | ¥ 1,990 | 现货 | ||
100 mg | ¥ 2,970 | 现货 | ||
200 mg | ¥ 4,280 | 现货 | ||
500 mg | ¥ 6,680 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 638 | 现货 |
产品描述 | Sivelestat (ONO5046) is a potent and selective inhibitor of neutrophil elastase with IC50 of 44 nM. |
靶点活性 | Neutrophil elastase:44 nM. |
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. |
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. |
别名 | ONO5046, EI546, 西维来司他, LY544349 |
分子量 | 434.46 |
分子式 | C20H22N2O7S |
CAS No. | 127373-66-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 80 mg/mL (184.1 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 80 mg/mL (184.1 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.3017 mL | 11.5085 mL | 23.0171 mL | 57.5427 mL |
5 mM | 0.4603 mL | 2.3017 mL | 4.6034 mL | 11.5085 mL | |
10 mM | 0.2302 mL | 1.1509 mL | 2.3017 mL | 5.7543 mL | |
20 mM | 0.1151 mL | 0.5754 mL | 1.1509 mL | 2.8771 mL | |
50 mM | 0.046 mL | 0.2302 mL | 0.4603 mL | 1.1509 mL | |
100 mM | 0.023 mL | 0.1151 mL | 0.2302 mL | 0.5754 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Sivelestat 127373-66-4 Microbiology/Virology Others Proteases/Proteasome SARS-CoV Serine Protease ONO5046 Inhibitor ischemia LY-544349 inhibit LY 544349 Acute EI546 reperfusion 西维来司他 EI-546 EI 546 SARS coronavirus injury ONO 5046 Elastase lung ONO-5046 LY544349 inhibitor