Sivelestat

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。

产品编号 T6986Cas号 127373-66-4

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Sivelestat

产品编号 T6986别名 ONO5046, EI546, LY544349, 西维来司他Cas号 127373-66-4

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规格	价格	库存
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 x 10 mM (in DMSO)	¥ 638	现货

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"Sivelestat"的相关化合物库

产品介绍

生物活性

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 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。
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, LY544349, 西维来司他

化学信息

分子量	434.46
分子式	C₂₀H₂₂N₂O₇S
CAS No.	127373-66-4

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

Ethanol: 80 mg/mL (184.1 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 45 mg/mL (103.58 mM)

溶液配制表

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.3017 mL	11.5085 mL	23.0171 mL	115.0854 mL
5 mM	0.4603 mL	2.3017 mL	4.6034 mL	23.0171 mL
10 mM	0.2302 mL	1.1509 mL	2.3017 mL	11.5085 mL
20 mM	0.1151 mL	0.5754 mL	1.1509 mL	5.7543 mL
50 mM	0.0460 mL	0.2302 mL	0.4603 mL	2.3017 mL
100 mM	0.0230 mL	0.1151 mL	0.2302 mL	1.1509 mL