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PNU-120596

Catalog No.
B1615
α7 nAChR modulator,positive allosteric
Grouped product items
SizePriceStock Qty
50mg
$190.00
In stock
10mg
$50.00
In stock
200mg
$610.00
In stock

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Background

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.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt311.73
Cas No.501925-31-1
FormulaC13H14ClN3O4
Solubility≥31.2mg/mL in DMSO
Chemical Name1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methyl-1,2-oxazol-3-yl)urea
SDFDownload SDF
Canonical SMILESCC1=CC(=NO1)NC(=O)NC2=CC(=C(C=C2OC)OC)Cl
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description PNU-120596 is a positive allosteric modulator of α7 nAChR with an EC50 value of 216 nM.
Targets α7 nAChR          
IC50 216 nM(EC50)          

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