1、Product Data SheetNimesulideCat. No.: HY-B0363CAS No.: 51803-78-2分式: CHNOS分量: 308.31作靶點(diǎn): COX作通路: Immunology/Inflammation儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (324.35 mM)H2O : 100 M；Nimesulide 具有抗炎、痛、解熱的作。IC & Target COX-20.07-70 M (IC50)體外研究

2、 Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 M in a time-dependent manner, but it shows weakeffect on COX-1 (IC50 100 M)1. Nimesulide (10 M) effectively decreases VEGF in endometrium cancer cells, andshows no effect on that in normal cells. Nimesulide (10 and 50 M) dramatically

3、 decreases MCP-1 levels in normalcell, and such an effect is also observed with 10 M in cancer cells. In addition, Nimesulide (50 M) potently affects IL-8 level in normal cells, but causes no changes in cancer cells3.體內(nèi)研究 Nimesulide (3 and 10 mg/kg, i.p.) effectively blocks fever induced by i.p. inj

4、ection of LPS in rats. Nimesulide (3 mg/kg,i.p.) potently reduces fever response induced by IL-1, IL-6 or TNF-, but does not prevent the initial rise in the febrileresponse induced by arachidonic acid. Nimesulide also significantly reduces PGE2 levels and PGF2 levels in thecerebrospinal fluid of the

5、 LPS-stimulated animals, and inhibits the increase in plasma TNF- by 97%2.PROTOCOLCell Assay 3 5105 viable cells are carefully dislodged with sterile Pasteur pipettes, transferred into new flasks and incubated withtwo different doses of Nimesulide (10 and 50 M) for another 24 h. Incubations for diff

6、erent doses of Nimesulideare repeated three times. The culture supernatant is then collected and stored in small aliquots at -70C until studied.VEGF, MCP-1 and IL-8 concentrations are determined by sandwich quantitative enzyme immunoassay (ELISA) usingcommercial kits3.MCE has not independently confi

7、rmed the accuracy of these methods. They are for reference only.Animal Rats2Administration 2 In the initial experiments, rats are pre-treated with intraperitoneal injections of 1, 3 or 10 mg/kg doses of Nimesulide, diluted in a 5% cremophor vehicle, or 2 mg/kg of indomethacin diluted in tris(hydroxi

8、metyl)-aminomethane-HCl (TRIS), pH 8.2, 30 min prior to an i.p. injection of LPS (50 g/kg). Control animals receive theappropriate vehicle plus saline (1 mL/200 g, i.p.). The dose of 3 mg/kg of Nimesulide is chosen for the remainingexperiments. In another set of experiments, rats are pretreated with

9、 an i.p. injection of Nimesulide (3 mg/kg) orindomethacin (2 mg/kg), diluted in the appropriate vehicles, 30 min prior to an i.c.v. injection (2 L over 1 min) of IL-1 (3.12 ng), IL-6 (300 ng), TNF- (250 ng), arachidonic acid (50 g), MIP-1 (500 ng), PGE2 (250 ng), PGF2 (250 ng),CRF (2 g) or ET-1 (1 p

10、mol). Control animals receive the appropriate vehicles (1 mL/200 g, i.p.) and sterile saline (2 Lover 1 min, i.c.v.). All the drugs are injected between 10:00 and 11:00 AM to avoid circadian rhythm variations2.MCE has not independently confirmed the accuracy of these methods. They are for reference

11、only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn)Page 2 of 3 www.MedChemE J Hazard Mater. 2015 May 30;289:18-27. Phys Chem Chem Phys. 2017 Aug 23;19(33):22099-22110. J Phys Chem Solids. 2017 October;109:117-123. Institute of Chemistry, Federal University of Rio Grande do Sul (UFRGS). 2017 Nov.See more customer validations on HYPERL

12、INK www.MedChemE www.MedChemEREFERENCES1. Vago T, et al. Effect of nimesulide action time dependence on selectivity towards prostaglandin G/H synthase/cyclooxygenase activity.Arzneimittelforschung. 1995 Oct;45(10):1096-8.2. Werner MF, et al. Nimesulide-induced antipyresis in rats involves both cyclooxygenase-dependent and independent mechanisms. Eur J Pharmacol. 2006Aug 14;543(1-3):181-9.3. Gen S, et al. The effect of COX-2 inhibitor, nimesulide, on angiogenetic factors in primary endometrial carcinoma cell culture. Clin Exp Med. 2007Mar;7(1):6-10.McePdfHeightCaution: Product