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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.
PHA 568487 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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
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
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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.
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
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.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.