Nimesulide-R805-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENimesulideCat. No.: HY-B0363CAS No.: 51803-78-2Synonyms: R805分式: CHNOS分量: 308.31作靶点: COX作通路: Immunology/Inflammation储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (324.35 mM)H2O

2、: 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.11 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (8.11 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Nimesulide种有选择性的 COX-2 抑制剂，对其抑制具有时间依赖性，IC50 值为 70 nM-70 M，但对COX-

3、1 的作弱，IC50 值 100 M；Nimesulide 具有抗炎、痛、解热的作。IC50 & Target COX-20.07-70 M (IC50)体外研究 Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 M in a time-dependent manner, but itshows weak effect on COX-1 (IC50 100 M) 1. Nimesulide (10 M) effectively decreases VEGF inendometrium cancer cells,

4、and shows no effect on that in normal cells. Nimesulide (10 and 50 M)dramatically decreases MCP-1 levels in normal cell, and such an effect is also observed with 10 M in cancercells. In addition, Nimesulide (50 M) potently affects IL-8 level in normal cells, but causes no changes incancer cells 3.体内

5、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-1, IL-6 or TNF-, but does not prevent theinitial rise in the febrile response induced by arachidonic acid. Nimesulide also s

6、ignificantly reduces PGE2levels and PGF2 levels in the cerebrospinal fluid of the LPS-stimulated animals, and inhibits the increase inplasma TNF- by 97% 2.PROTOCOLCell Assay 3 5105 viable cells are carefully dislodged with sterile Pasteur pipettes, transferred into new flasks andincubated with two d

7、ifferent doses of Nimesulide (10 and 50 M) for another 24 h. Incubations for differentdoses of Nimesulide are repeated three times. The culture supernatant is then collected and stored in smallaliquots at -70C until studied. VEGF, MCP-1 and IL-8 concentrations are determined by sandwichquantitative

8、enzyme immunoassay (ELISA) using commercial kits 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats 2Administration 2 In the initial experiments, rats are pre-treated with intraperitoneal injections of 1, 3 or 10 mg/kg doses ofNimesulide, dil

9、uted in a 5% cremophor vehicle, or 2 mg/kg of indomethacin diluted in tris(hydroximetyl)-aminomethane-HCl (TRIS), pH 8.2, 30 min prior to an i.p. injection of LPS (50 g/kg). Control animals receivethe appropriate vehicle plus saline (1 mL/200 g, i.p.). The dose of 3 mg/kg of Nimesulide is chosen for

10、 theremaining experiments. In another set of experiments, rats are pretreated with an i.p. injection of Nimesulide(3 mg/kg) or indomethacin (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), arachidoni

11、c acid (50 g), MIP-1 (500 ng),PGE2 (250 ng), PGF2 (250 ng), CRF (2 g) or ET-1 (1 pmol). Control animals receive the appropriatevehicles (1 mL/200 g, i.p.) and sterile saline (2 L over 1 min, i.c.v.). All the drugs are injected between 10:002/3 Master of Small Molecules 您边的抑制剂师www.MedChemEand 11:00 A

12、M to avoid circadian rhythm variations 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 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 C

13、hemistry, Federal University of Rio Grande do Sul (UFRGS). 2017 Nov.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Vago T, et al. Effect of nimesulide action time dependence on selectivity towards prostaglandin G/H synthase/cyclooxygenase activity.Arzneimittelforschung. 1995 O

14、ct;45(10):1096-8.2. Werner MF, et al. Nimesulide-induced antipyresis in rats involves both cyclooxygenase-dependent and independent mechanisms. Eur JPharmacol. 2006 Aug 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 ExpMed. 2007 Mar