| 产品描述： | Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease |
| 靶点： |
muscarinic receptor;AChR |
| 体外研究： |
Xanomeline stimulates phosphoinositide (PI) hydrolysis in the A9 L m1 cells. Xanomeline inhibits [3H]-pirenzepine ([3H]-PZ) and [3H]-oxotremorine-M ([3H]-OXO-M) binding to rat brain with Kis of 7 and 3 nM, respectively |
| 体内研究： |
Xanomeline robustly stimulates in vivo PI hydrolysis and the effect is blocked by muscarinic antagonists, demonstrating mediation by muscarinic receptors. In mice the ED100 for Xanomeline-induced stimulation of [3H]-IP accumulation is 54 μmole/kg in hippocampus. And in rats the ED100 for Xanomeline-induced stimulation of [3H]-IP accumulation is 8.1 μmole/kg in hippocampus. Animal Model: Male CF1 mice weighing 18-20 g are injected [3H]-myoinositol Dosage: 8.1-81 μmole/kg Administration: S.c. injections; 1 h prior to killing and 1 h after the administration Result: Increased accumulation in a dose-related manner up to 130%, 75%, 60% above lithium levels in hippocampus, cortex and neostriatum, respectively. And did not increase accumulation of [3H]-IP in the brain stem. Induced salivation, tremor and hypothermia in mice with the ED50 of 13.7±0.8 μmole/kg. Animal Model: Rats are injected [3H]-myoinositol Dosage: 2.7-81 μmole/kg Administration: S.c. injections; 1 h prior to killing and 1 h after the administration Result: Increased [3H]-IP formation dose dependently in hippocampus up to 221% above lithium control. |
| 参考文献： |
1. F P Bymaster, et al. Xanomeline Compared to Other Muscarinic Agents on Stimulation of Phosphoinositide Hydrolysis in Vivo and Other Cholinomimetic Effects. Brain Res. 1998 Jun 8; 795(1-2):179-90. |
| 溶解性： |
soluble in DMSO |
| 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 |
2.692 ml |
13.461 ml |
26.921 ml |
| 5 mM |
0.538 ml |
2.692 ml |
5.384 ml |
| 10 mM |
0.269 ml |
1.346 ml |
2.692 ml |
| 50 mM |
0.054 ml |
0.269 ml |
0.538 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