Potent and selective P2X7 antagonist (pIC50 values are 8.3, 7.5 and 7.2 for human, mouse and rat receptors respectively). Selective over a panel of 50 other receptors, ion channels and transporters. Reduces BzATP-induced IL-1β release from monocytes in vitro and from rat brain in vivo. Attenuates amphetamine-induced hyperactivity in rats. Brain penetrant.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 488.64. 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||2.05 mL||10.23 mL||20.46 mL|
|5 mM||0.41 mL||2.05 mL||4.09 mL|
|10 mM||0.2 mL||1.02 mL||2.05 mL|
|50 mM||0.04 mL||0.2 mL||0.41 mL|
References are publications that support the biological activity of the product.
Bhattacharya et al (2013) Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567. Br.J.Pharmacol. 170 624 PMID: 23889535
Letavic et al (2013) Synthesis and pharmacological characterization of two novel, brain penetrating P2X7 antagonists. ACS Med.Chem.Lett. 12 419 PMID: 24900687
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Keywords: JNJ 47965567, JNJ 47965567 supplier, JNJ47965567, potent, selective, p2x7, purinergics, antagonists, brain, penetrant, P2X, Receptors, 5299, Tocris Bioscience
Citations for JNJ 47965567
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Reviews for JNJ 47965567
Average Rating: 4 (Based on 2 Reviews.)
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I have used this product emulsified in 30% sulphoxymethylester, and injected them sub-cutaneously to study IL-1beta release mechanism in the hippocampus of the brain. I am currently working on its effect on hippocampal neurons in culture.
Followed publication by Bhattacharya et al, Br J Pharmacol. 2013 Oct;170(3):624-40. doi: 10.1111/bph.12314 for in vivo and in vitro usage.
Used to block a potentially P2X7-dependent process, but no effect was observed. No positive control so unsure if the drug actually blocked its target. More experiments needed.
Literature in this Area
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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.