PHA 543613 hydrochloride

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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 (7)
Reviews (1)
Literature (3)

Biological Activity for PHA 543613 hydrochloride

PHA 543613 hydrochloride is a 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.

Compound Libraries for PHA 543613 hydrochloride

PHA 543613 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for PHA 543613 hydrochloride

M. Wt 307.78
Formula C15H17N3O2.HCl
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1586767-92-1
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PHA 543613 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 30.78 100
DMSO 7.69 25

Preparing Stock Solutions for PHA 543613 hydrochloride

The following data is based on the product molecular weight 307.78. 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.

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 for PHA 543613 hydrochloride

Certificate of Analysis / Product Datasheet
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References for PHA 543613 hydrochloride

References are publications that support the biological activity of the product.

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: 1849016


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Keywords: PHA 543613 hydrochloride, PHA 543613 hydrochloride supplier, Potent, selective, α7, alpha7, a7, nAChR, agonists, Nicotinic, Receptors, Acetylcholine, PHA543613, hydrochloride, Pfizer, 478149-53-0, (a7), 3092, Tocris Bioscience

7 Citations for PHA 543613 hydrochloride

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

Sérriàre et al (2015) Assessment of the Protection of DArgic 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

Bali et al (2019) Facilitation and inhibition of firing activity and N-methyl-D-aspartate-evoked responses of CA1 hippocampal pyramidal cells by alpha7 nicotinic acetylcholine receptor selective compounds in vivo. Sci Rep 9 9324 PMID: 31249369

Wang et al (2012) Electroacupuncture pretreatment attenuates cerebral ischemic injury through α7 nicotinic acetylcholine receptor-mediated inhibition of high-mobility group box 1 release in rats. J Neuroinflammation 9 24 PMID: 22277256

Bali et al (2019) Cognitive enhancer effects of low Mem. doses are facilitated by an alpha7 nicotinic acetylcholine receptor agonist in scopolamine-induced amnesia in rats. Front Pharmacol 10 73 PMID: 30804787


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Reviews for PHA 543613 hydrochloride

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Cognitive enhancer effect of PHA 543613 in rat behavioral tests.
By Zsolt Bali on 02/14/2018
Assay Type: In Vivo
Species: Rat

We used PHA 543613 in behavioral pharmacology experiments and tested its cognitive enhancer effect. PHA 543613 was found effective in different behavioral paradigms, and in different models of cognitive impairment. For instance, PHA 543613 dose-dependently reversed scopolamine induced transient amnesia in the spontaneous alternation (t-maze) task of rats.

Sometimes we experienced poor solubility in physiological saline. Slight warming and ultrasonics might help.

PMID: 25447295

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

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.

Alzheimer's Disease Poster

Alzheimer's Disease Poster

Alzheimer's disease (AD) is a debilitating and progressive neurodegenerative disease and the most common cause of dementia, affecting approximately 30% of individuals aged over 85 years. This poster summarizes the cellular and molecular mechanisms of AD.

Learning & Memory Poster

Learning & Memory Poster

Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.