PHA 568487

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Cat.No. 3134 - PHA 568487 | C16H20N2O3.C4H4O4 | CAS No. 527680-57-5
Description: α7-selective 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)
Datasheet
Citations (2)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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View all Nicotinic (α7) Receptor Agonists

Keywords: PHA 568487, supplier, α7, alpha7, selective, agonists, a7, Nicotinic, Receptors, Acetylcholine, nAChR, PHA568487, Nicotinic, (a7), Receptors, Nicotinic, (a7), Receptors, 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? If so please let us know.

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Pathways for PHA 568487

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