西维来司他 T6986

Product Introduction
Bioactivity


英文名: Sivelestat

描述: 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。

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: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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)


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

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相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Approved Drug Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Anti-Fibrosis Compound Library | Anti-Viral Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途