| 产品描述： | SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K>i=260 nM) and acts as full agonist in functional Ca2+ flux studies (EC50=1.6 μM). SEN 12333 is used for AD and schizophrenia research |
| 靶点： |
nAChR;AChR |
| 体外研究： |
In whole-cell patch-clamp recordings, SEN12333 activates peak currents and maximal total charges similar to acetylcholine (EC50= 12 μM). SEN12333 displays functional antagonism at histamine H3 receptors (IC50=103 nM) and weak agonist activity at human ganglionic α3 nAChRs (IC50=8.5 μM) |
| 体内研究： |
SEN12333 (intraperitoneal injection; 3 mg/kg) improves episodic memory in a novel object recognition task in rats in conditions of spontaneous forgetting as well as cognitive disruptions induced via glutamatergic or cholinergic mechanisms. SEN12333 also prevents a scopolamine-induced deficit in a passive avoidance task |
| 参考文献： |
1. Corinne Beinat, et al. The Recent Development of α7 Nicotinic Acetylcholine Receptor (nAChR) Ligands as Therapeutic Candidates for the Treatment of Central Nervous System (CNS) Diseases.Curr Pharm Des. 2016;22(14):2134-51. 2. Renza Roncarati, et al. Procognitive and neuroprotective activity of a novel alpha7 nicotinic acetylcholine receptor agonist for treatment of neurodegenerative and cognitive disorders. J Pharmacol Exp Ther. 2009 May;329(2):459-68. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.946 ml |
14.731 ml |
29.461 ml |
| 5 mM |
0.589 ml |
2.946 ml |
5.892 ml |
| 10 mM |
0.295 ml |
1.473 ml |
2.946 ml |
| 50 mM |
0.059 ml |
0.295 ml |
0.589 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