T83862 |
SEN 12333 |
源叶(MedMol) | 98% |
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)