首页 Proteases/Proteasome Serine Protease Sivelestat
Sivelestat
编号 T6986     别名: LY544349, ONO5046, EI546, ONO5046, LY544349 EI546
CAS 127373-66-4     分子式 C20H22N2O7S     分子量 434.46
靶点: neutrophil elastase;
Sivelestat is a potent and selective inhibitor of neutrophil elastase with IC50 of 44 nM.
选择批次  
规格 库存 单价 数量
5 mg 上海现货 331.00
10 mg 上海现货 595.00
25 mg 上海现货 1071.00
50 mg 上海现货 2040.00
100 mg 上海现货 3060.00
200 mg 上海现货 5251.00
1 mL * 10 mM (in DMSO) 上海现货 660.00
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生物活性

产品描述

Sivelestat is a potent and selective inhibitor of neutrophil elastase with IC50 of 44 nM.

靶点活性

neutrophil elastase,

实验溶液

5% DMSO+40% PEG 300+5% Tween 80+ddWater: 23mg/mL

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.

细胞系: TMK-1 gastric carcinoma cells

动物实验

Animal Models: Male Sprague-Dawley rats. Formulation: Saline. Dosages: 50 or 100 mg/kg. Administration: i.p.

动物模型:

化学信息

分子量

434.46

分子式

C20H22N2O7S

CAS

127373-66-4

溶解度

DMSO: 80 mg/mL (184.1 mM)

Ethanol: 80 mg/mL (184.1 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.302 ml 11.509 ml 23.017 ml
5 mM 0.46 ml 2.302 ml 4.603 ml
10 mM 0.23 ml 1.151 ml 2.302 ml
50 mM 0.046 ml 0.23 ml 0.46 ml
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