PHA 543613 hydrochloride

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Cat.No. 3092 - PHA 543613 hydrochloride | C15H17N3O2.HCl | CAS No. 478149-53-0
Description: Potent and selective α7 nAChR agonist
Chemical Name: N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-furo[2,3-c]pyridine-5-carboxamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Literature

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.

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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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:


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3 Citations for PHA 543613 hydrochloride

Citations are publications that use Tocris products. Selected citations for PHA 543613 hydrochloride include:

Foucault-Fruchard (2017) Neuroprotective effect of the alpha 7 nicotinic receptor agonist PHA 543613 in an in vivo excitotoxic adult rat model. Neuroscience 356 52 PMID: 28527955

Sérriàre et al (2015) Assessment of the Protection of Dopaminergic Neurons by an α7 Nicotinic Receptor Agonist, PHA 543613 Using [(18)F]LBT-999 in a Parkinson's Disease Rat Model. Cell Death Differ 2 61 PMID: 26389120

Macpherson et al (2014) The α7 nicotinic receptor agonist PHA-543613 hydrochloride inhibits Porphyromonas gingivalis-induced expression of interleukin-8 by oral keratinocytes. Front Med (Lausanne) 63 557 PMID: 24609617


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