S83161 |
Xanomeline (oxalate) |
源叶(MedMol) | ≥98% |
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- 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: 2-8℃;充氩;干燥
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)