Biological Activity
Potent α7 nAChR agonist that displays selectivity over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. Positively influences sensory gating and memory in in vivo models of schizophrenia. Orally active and brain penetrant.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 307.78 |
| Formula | C15H17N3O2.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 478149-53-0 |
| PubChem ID | 56972222 |
| InChI Key | YMTPSZUBRSEWNY-ZOWNYOTGSA-N |
| Smiles | O=C(C2=NC=C(OC=C3)C3=C2)N[C@@H]1C4CCN(CC4)C1.Cl |
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 | 7.69 | 25 | |
| water | 30.78 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 307.78. 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 | 3.25 mL | 16.25 mL | 32.49 mL |
| 5 mM | 0.65 mL | 3.25 mL | 6.5 mL |
| 10 mM | 0.32 mL | 1.62 mL | 3.25 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.65 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Wishka et al (2006) Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the α7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia; synthesis and st J.Med.Chem. 49 4425 PMID: 16821801
Faghih et al (2008) Allosteric modulators of the α7 nicotinic acetylcholine receptor. J.Med.Chem. 51 701 PMID: 18198823
Acker et al (2008) Discovery of N-[3R,5R)-1-azabicyclo[3.2.1]ocy-3-yl]furo-[2,3-c]pyridine-5-carboxamide as an agonist of the α7 nicotinic acetylcholine receptor: in vitro and in vivo activity. Bioorg.Med.Chem.Letts. 18 3611 PMID:
Keywords: PHA 543613 hydrochloride, supplier, Potent, selective, α7, alpha7, a7, nAChR, agonists, Nicotinic, Receptors, Acetylcholine, PHA543613, hydrochloride, Pfizer, Nicotinic, (a7), Receptors, Nicotinic, (a7), Receptors, Tocris Bioscience
