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Submit ReviewPHA 568487
Description: Selective α7 nAChR agonist
Chemical Name: N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-2,3-dihydro-1,4-benzodioxin-6-carboxamide fumarate
Purity: ≥99% (HPLC)
Biological Activity for PHA 568487
PHA 568487 is an 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 for PHA 568487
PHA 568487 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for PHA 568487
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PHA 568487
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 40.44 | 100 | |
| DMSO | 40.44 | 100 |
Preparing Stock Solutions for PHA 568487
The following data is based on the product molecular weight 404.41. Batch specific molecular weights may vary from batch to batch due to the degree 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 for PHA 568487
References for PHA 568487
References are publications that support the biological activity of the product.
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
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Keywords: PHA 568487, PHA 568487 supplier, α7, alpha7, selective, agonists, a7, Nicotinic, Receptors, Acetylcholine, nAChR, PHA568487, (a7), 3134, Tocris Bioscience
2 Citations for PHA 568487
Citations are publications that use Tocris products. Selected citations for PHA 568487 include:
Foucault-Fruchard (2017) Neuroprotective effect of the alpha 7 nicotinic receptor agonist PHA 543613 in an n vivo excitotoxic adult rat model. Neuroscience 356 52 PMID: 28527955
Su et al (2013) Dysfunction of inflammation-resolving pathways is associated with exaggerated postoperative cognitive decline in a rat model of the metabolic syndrome. Mol Med 18 1481 PMID: 23296426
Do you know of a great paper that uses PHA 568487 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Nicotinic ACh Receptors Scientific Review
Updated in 2014, this review by Sue Wonnacott summarizes the diverse structure and function of nicotinic acetylcholine receptors and gives an in-depth review of the ligands available for nAChR research. Compounds available from Tocris are listed.
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