| 产品描述： | Tolmetin sodium dihydrate is an orally active and potent COX inhibitor with IC50s of 0.35 µM and 0.82 µM human COX-1 and COX-2, respectively. Tolmetin sodium dihydrate is a non-steroidal anti-inflammatory drug (NSAID) |
| 靶点： |
Human COX-1:0.35 μM (IC50);Human COX-2:0.82 μM (IC50) |
| 体内研究： |
Tolmetin sodium dihydrate (30,100 mg/kg; gavage; single dose or twice daily for 3 and 14 days) shows maximal ulcerogenic effect 4 h after the single dose, while potently decreases after 3 and 14 days of repeated administration in male Wistar rats weighing 180-200 g. Tolmetin causes gastric lesions in 100 mg/kg. Tolmetin sodium dihydrate (5 mg/kg twice a day for 5 days) pre-treatment considerably attenuates quinolinic acid (QA)-induced neurotoxicity |
| 参考文献： |
1. T D Warner, et al. Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis. Proc Natl Acad Sci U S A. 1999 Jun 22;96(13):7563-8. 2. Morini G, et al. Morphological features of rat gastric mucosa after acute and chronic treatment with amtolmetin guacyl: comparison with non-selective and COX-2-selective NSAIDs. Digestion. 2003;68(2-3):124-32. Epub 2003 Nov 7. 3. Dairam A, et al. Non-steroidal anti-inflammatory agents, tolmetin and sulindac, attenuate oxidative stress in rat brain homogenate and reduce quinolinic acid-induced neurodegeneration in rat hippocampal neurons. Metab Brain Dis. 2006 Sep;21(2-3):221-33. 4. DADAŞ, Yakup, et al. Synthesis and anticancer activity of some novel tolmetin thiosemicarbazides. Marmara Pharmaceutical Journal 19(3) • April 2015 5. 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. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.172 ml |
15.858 ml |
31.716 ml |
| 5 mM |
0.634 ml |
3.172 ml |
6.343 ml |
| 10 mM |
0.317 ml |
1.586 ml |
3.172 ml |
| 50 mM |
0.063 ml |
0.317 ml |
0.634 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京