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Nimesulide

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Chemical Structure| 51803-78-2 同义名 : R805
CAS号 : 51803-78-2
货号 : A370794
分子式 : C13H12N2O5S
纯度 : 98%
分子量 : 308.31
MDL号 : MFCD00079470
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(340.57 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • COX-2

    COX-2, IC50:26 μM
描述 Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties[3]. Nimesulide, but not indomethacin, reduced the fever induced by MIP-1alpha, PGF(2alpha), CRF or ET-1. Plasma TNF-alpha levels in LPS-treated rats were also reduced by nimesulide[4]. 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[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02466581 Rheumatoid Arthritis Phase 4 Recruiting December 2021 Sweden ... 展开 >> Karolinska Institutet Recruiting Stockholm, Sweden, 171 76 Contact: Ronald van Vollenhoven, MD, prof    +46(8)51776077    ronald.van.vollenhoven@ki.se    Contact: Monica Ryden Aulin, PhD    +46(8)51771110    monica.ryden.aulin@ki.se 收起 <<
NCT02563756 Knee Osteoarthritis Not Applicable Recruiting September 2022 Sweden ... 展开 >> Karolinska University Hospital Recruiting Stockholm, Sweden Contact: Carl Aulin, MD       carl.aulin@karolinska.se    Contact: Nicolas Martinez, MD    +46709900089    nicolas.martinez-carranza@karolinska.se 收起 <<
NCT03104985 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.24mL

0.65mL

0.32mL

16.22mL

3.24mL

1.62mL

32.43mL

6.49mL

3.24mL
参考文献

[1]Rainsford KD; Members of the Consensus Report Group on Nimesulide. Nimesulide -- a multifactorial approach to inflammation and pain: scientific and clinical consensus. Curr Med Res Opin. 2006 Jun;22(6):1161-70.

[2]Bernareggi A. Clinical pharmacokinetics of nimesulide. Clin Pharmacokinet. 1998 Oct;35(4):247-74.

[3]Vago T, Bevilacqua M, Norbiato G. Effect of nimesulide action time dependence on selectivity towards prostaglandin G/H synthase/cyclooxygenase activity. Arzneimittelforschung.1995;45(10):1096-1098

[4]Werner MF, Souza GE, Zampronio AR. Nimesulide-induced antipyresis in rats involves both cyclooxygenase-dependent and independent mechanisms. Eur J Pharmacol. 2006;543(1-3):181-189

[5]Genç S, Attar E, Gürdöl F, Kendigelen S, Bilir A, Serdaroğlu H. The effect of COX-2 inhibitor, nimesulide, on angiogenetic factors in primary endometrial carcinoma cell culture. Clin Exp Med. 2007;7(1):6-10