Biological Activity
Agonist of the α7 nicotinic acetylcholine receptor (Ki values are 44 and 2800 for α7 and 5-HT3 respectively, IC50 values are > 100 μM for α3β4 and α1β1δγ respectively, and % inhibition is < 1 and 5% for α4β2 and hERG respectively). Orally active and brain penetrant.
Compound Libraries
PHA 568487 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 404.41 |
| Formula | C16H20N2O3.C4H4O4 |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 527680-57-5 |
| PubChem ID | 56972212 |
| InChI Key | QYQZUGYJVHHHEE-QDSMGTAFSA-N |
| Smiles | O=C(C3=CC=C(OCCO4)C4=C3)N[C@@H]1C2CCN(CC2)C1.O=C(/C=C/C(O)=O)O |
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 | 40.44 | 100 | |
| water | 40.44 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 404.41. 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 | 2.47 mL | 12.36 mL | 24.73 mL |
| 5 mM | 0.49 mL | 2.47 mL | 4.95 mL |
| 10 mM | 0.25 mL | 1.24 mL | 2.47 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Walker et al (2006) Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as α7 nicotinic acetylcholine receptor agonists. Bioorg.Med.Chem. 14 8219 PMID: 17011782
Keywords: PHA 568487, supplier, α7, alpha7, selective, agonists, a7, Nicotinic, Receptors, Acetylcholine, nAChR, PHA568487, Nicotinic, (a7), Receptors, Nicotinic, (a7), Receptors, Tocris Bioscience
