Biological Activity
Positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors (EC50 = 216 nM), with no detectable effect on α4β2, α3β4 and α9α10 receptors. Active in vivo following systemic administration. Neuroprotective in an in vivo model of transient focal cerebral ischemia.
Compound Libraries
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Technical Data
| M. Wt | 311.72 |
| Formula | C13H14ClN3O4 |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 501925-31-1 |
| PubChem ID | 311434 |
| InChI Key | CEIIEALEIHQDBX-UHFFFAOYSA-N |
| Smiles | COC1=CC(OC)=C(Cl)C=C1NC(=O)NC1=NOC(C)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 31.17 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 311.72. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.21 mL | 16.04 mL | 32.08 mL |
| 5 mM | 0.64 mL | 3.21 mL | 6.42 mL |
| 10 mM | 0.32 mL | 1.6 mL | 3.21 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
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References
References are publications that support the products' biological activity.
Hurst et al (2005) A novel positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J.Neurosci. 25 4396 PMID: 15858066
Timmermann et al (2007) An allosteric modulator of the α7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J.Pharmacol.Exp.Ther. 323 294 PMID: 17625074
Kalappa et al (2013) A positive allosteric modulator of α7 nAChRs augments neuroprotective effects of endogenous nicotinic agonists in cerebral ischemia. Br.J.Pharmacol. [Epub ahead of print] PMID: 23713819
Keywords: PNU 120596, supplier, Positive, allosteric, modulators, α7, alpha7, a7, nAChR, active, vivo, Nicotinic, Receptors, Acetylcholine, PNU120596, Nicotinic, (a7), Receptors, Nicotinic, (a7), Receptors, Tocris Bioscience
