Tolmetin-sodium-dihydrate - COX 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETolmetin sodium dihydrateCat. No.: HY-B1489CAS No.: 64490-92-2分式: CHNNaO分量: 315.3作靶點(diǎn): COX作通路: Immunology/Inflammation儲(chǔ)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) H2O : 100 mg/mL (317.16 mM)* me

2、ans soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.1716 mL 15.8579 mL 31.7158 mL5 mM 0.6343 mL 3.1716 mL 6.3432 mL10 mM 0.3172 mL 1.5858 mL 3.1716 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Tolmetin sodium dihydrate種甾體抗炎劑，為選擇性的 COX 抑制劑。

3、IC50 & Target COX體外研究Tolmetin sodium dihydrate is a non-steroidal antiinflammatory agent. Tolmetin (0-100 M) shows no effect onosteoblast growth 2. Tolmetin (0.25 mM) dose not attenuate lipid peroxidation in rat brain homogenate.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemETolmetin (0.25, 0.5, 0

4、.75, 1 mM) shows radical scavenging properties but without superoxide aniongeneration in rat brain homogenat 3.體內(nèi)研究 Tolmetin (100 mg/kg) causes gastric lesions, and shows maximal ulcerogenic effect 4 h after the single dose,while potently decreases after 3 and 14 days of repeated administration. Tol

5、metin produces obviousendothelial damage and inflammatory cell infiltration 1. Tolmetin (5 mg/kg, i.p., twice a day for 5 days) hasno effect on n NMDA receptor binding in rats 3.PROTOCOLAnimal Rats 1Administration 1 After 2 weeks of acclimatization, rats are randomized to different groups and given

6、the non-selective COXinhibitors, amtolmetin guacyl (AMG) (50 and 150 mg/kg) and Tolmetin (30 and 100 mg/kg) as well as theselective COX-2 inhibitor, celecoxib (CXIB; 20 and 60 mg/kg). The compounds are suspended in 1%carboxymethylcellulose (CMC) immediately before use and administered by gavage in a

7、 10-mL/kg volume.Control groups receive CMC in the same volume. Rats from each group are divided into 3 subgroups,consisting each of at least 10 animals. Subgroups are dosed either with a single dose (acute treatmentgroup) or twice daily for 3 and 14 days (chronic treatment groups). To ensure that a

8、ll groups are dosed forthe same period of time, those receiving less than 14 days of NSAIDs are given CMC until they are due tostart the assigned treatment. Rats are killed by cervical dislocation 4 h after the last administration. Stomachsare immediately removed, opened along the lesser curvature a

9、nd gently rinsed 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Morini G, et al. Morphological features of rat gastric mucosa after acute and chronic treatment with amtolmetin guacyl: comparison withnon-selective and COX-2-selective NSAI

10、Ds. Digestion. 2003;68(2-3):124-32. Epub 2003 Nov 7.2. Etcheverry SB, et al. Three new vanadyl(IV) complexes with non-steroidal anti-inflammatory drugs (Ibuprofen, Naproxen and Tolmetin).Bioactivity on osteoblast-like cells in culture. J Inorg Biochem. 2002 Jan 1;88(1):94-100.3. Dairam A, et al. Non-steroidal anti-inflammatory agents, tolmetin and sulindac, attenuate oxidative stress in rat brain homogenate andreduce quinolinic acid-induced neurodegeneration in rat hippocampal neurons. Metab Brain Dis. 2006 Sep;21(2-3):221-33.McePdfHeightCaution: Product has not bee