Nimesulide,51803-78-2

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YZ剂描述：

产品名称：Nimesulide

产品别名：尼美舒利

英文别名：R805

靶点：COX

CAS：51803-78-2

纯度：>98%

外观：淡黄色粉末

保存方法：-20°C

描述：

Nimesulide is a relatively COX-2 selective inhibitor with IC50 of 26 μM.

溶解性：Ethanol ：7.7 mg/mL (25 mM)
DMSO ：30.8 mg/mL (100 mM)

体外研究：

Nimesulide is a selective COX-2 inhibitor, with IC₅₀s of 70 nM-70 μM in a time-dependent manner, but it shows weak effect on COX-1 (IC₅₀ >100 μM). Nimesulide (10 µM) effectively decreases VEGF in endometrium cancer cells, and shows no effect on that in normal cells. Nimesulide (10 and 50 µM) dramatically decreases MCP-1 levels in normal cell, and such an effect is also observed with 10 µM in cancer cells. In addition, Nimesulide (50 µM) potently affects IL-8 level in normal cells, but causes no changes in cancer cells.

体内研究：

Nimesulide (3 and 10 mg/kg, i.p.) effectively blocks fever induced by i.p. injection of LPS in rats. Nimesulide (3 mg/kg, i.p.) potently reduces fever response induced by IL-1β, IL-6 or TNF-α, but does not prevent the initial rise in the febrile response induced by arachidonic acid. Nimesulide also significantly reduces PGE2 levels and PGF2α levels in the cerebrospinal fluid of the LPS-stimulated animals, and inhibits the increase in plasma TNF-α by 97%.

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