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PNU-120596
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PNU-120596图片
CAS NO:501925-31-1
包装与价格:
包装价格(元)
10mg电议
50mg电议
200mg电议

产品介绍
PNU-120596 (NSC 216666) 是一种有效的选择性 α7 nAChR 正变构调节剂 (PMA),EC50 为 216 nM。
Cas No.501925-31-1
别名NSC 216666
化学名1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methyl-1,2-oxazol-3-yl)urea
Canonical SMILESCC1=CC(=NO1)NC(=O)NC2=CC(=C(C=C2OC)OC)Cl
分子式C13H14ClN3O4
分子量311.73
溶解度≥ 31.2mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

PNU-120596 is a positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptor (nAChR) [1].

PNU-120596 is a type 2 PAM. In cell-based assay, PNU-120596 significantly increases the Ca2+-mediated signal at the concentration of 3μM. It enhances the ACh-evoked Ca22+ flux with EC50 value of 216nM in SH-EP1 cells. PNU-120596 also markedly increases the agonist-evoked currents as well as the current duration in Xenopus oocytes. PNU-120596 is specific to α7nAChR over other neuronal nicotinic acetylcholine receptors. PNU-120596 also potentiates the ACh responses mediated byα7nAChRs in rat hippocampal interneurons. It is considered that PNU-120596 modulates the ACh-dependent increase via enhancing the excitatory effect of ACh on GABAergic interneurons. Furthermore, PNU-120596 is found to improve performance in rodent recognition memory model with increasing the phosphorylation of CREB [1, 2].

References:
[1] Hurst R S, Hajós M, Raggenbass M, et al. A novel positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. The Journal of neuroscience, 2005, 25(17): 4396-4405.
[2] Bertrand D, Gopalakrishnan M. Allosteric modulation of nicotinic acetylcholine receptors. Biochemical pharmacology, 2007, 74(8): 1155-1163.