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- 文献和实验
- 技术资料
- CAS号：
127373-66-4
- 规格：
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg/200mg/500mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥332.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥142.0 |
| 规格： | 5mg | 产品价格： | ￥280.0 |
| 规格： | 10mg | 产品价格： | ￥462.0 |
| 规格： | 25mg | 产品价格： | ￥856.0 |
| 规格： | 50mg | 产品价格： | ￥1592.0 |
| 规格： | 100mg | 产品价格： | ￥2376.0 |
| 规格： | 200mg | 产品价格： | ￥3424.0 |
| 规格： | 500mg | 产品价格： | ￥5344.0 |
Product Introduction
Bioactivity
| 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 通过抑制 NF-kB 的活性，降低炎症介质的水平，并在促炎细胞因子刺激的肝细胞中抑制 iNOS 基因的表达。此外，它还能抑制 NE 刺激下 TGF-α 的释放，从而抑制胃癌细胞的生长。 |
| 体内活性 | 给予sivelestat能够减轻小鼠急性肺损伤后的肺纤维化。Sivelestat还能减轻大鼠脓毒症相关的肾损伤。它通过阻断GAPDH/Siah1这一新型信号通路，从而减轻脊髓损伤的进展。 |
| 存储条件 | Keep away from direct sunlight,Keep away from moisture,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 80 mg/mL (184.14 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.6 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble) DMSO : 45 mg/mL (103.58 mM), Sonication is recommended. |
| 关键字 | Sivelestat | SerineProtease | Serine Protease | SARS-CoV | SARSCoV | SARS coronavirus | reperfusion | ONO-5046 | ONO 5046 | neutrophil elastase | LY-544349 | LY 544349 | lung | ischemia | injury | Inhibitor | inhibit | Elastase | EI-546 | EI 546 | Acute |
| 相关产品 | α-Cyclodextrin | Proteinase K | Chloroquine phosphate | Dexamethasone | Hydroxychloroquine | Subtilisin | Silymarin | Ritonavir | Ac-Ala-OH | Imidazole | Molnupiravir | AEBSF hydrochloride |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Anti-Viral Compound Library | Immunology/Inflammation Compound Library | Drug Repurposing Compound Library | Anti-Metabolism Disease Compound Library | Anti-Cancer Clinical Compound Library | Target-Focused Phenotypic Screening Library | Anti-Cancer Drug Library |
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￥142 - 5344
