Biological Activity
α7 nicotinic acetylcholine receptor (nAChR) agonist (EC50 = 1.6 μM, Ki = 260 nM at rat α7 nAChRs). Also displays functional antagonism at histamine H3 receptors (IC50 = 103 nM) and weak agonist activity at human ganglionic α3 nAChRs (IC50 = 8.5 μM). Neuroprotective in a rodent model of quisqualic acid-induced cholinergic degeneration. Brain penetrant and orally bioavailable.
Technical Data
| M. Wt | 339.43 |
| Formula | C20H25N3O2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 874450-44-9 |
| PubChem ID | 45484303 |
| InChI Key | XCHIZTUBUXZESJ-UHFFFAOYSA-N |
| Smiles | O=C(CCCCN3CCOCC3)NC(C=C2)=CC=C2C1=CC=CN=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 | 33.94 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 339.43. 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 | 2.95 mL | 14.73 mL | 29.46 mL |
| 5 mM | 0.59 mL | 2.95 mL | 5.89 mL |
| 10 mM | 0.29 mL | 1.47 mL | 2.95 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.59 mL |
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References
References are publications that support the products' biological activity.
Roncarati et al (2009) Procognitive and neuroprotective activity of a novel α7 nicotinic acetylcholine receptor agonist for treatment of neurodegenerative and cognitive disorders. J.Pharmacol.Exp.Ther. 329 459 PMID: 19223665
Beinat et al (2012) Consequences of linker length alteration of the α7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333. Bioorg.Med.Chem.Lett. 22 2380 PMID: 22410083
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