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Biological Activity for JNJ 47965567
JNJ 47965567 is a 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.
Compound Libraries for JNJ 47965567
Technical Data for JNJ 47965567
|Storage||Store at +4°C|
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 JNJ 47965567
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for JNJ 47965567
The following data is based on the product molecular weight 488.64. 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||2.05 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 for JNJ 47965567
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
1 Citation for JNJ 47965567
Citations are publications that use Tocris products. Selected citations for JNJ 47965567 include:
Uderhardt et al (2019) Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage. Cell 177 541 PMID: 30955887
Do you know of a great paper that uses JNJ 47965567 from Tocris? Please let us know.
Reviews for JNJ 47965567
Average Rating: 4.3 (Based on 3 Reviews.)
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DMSO dilution 100 μM
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.