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Submit ReviewJNJ 47965567
Description: Potent and selective P2X7 antagonist; brain penetrant
Chemical Name: 2-(Phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl-3-pyridinecarboxamide
Purity: ≥98% (HPLC)
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
JNJ 47965567 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for JNJ 47965567
| M. Wt | 488.64 |
| Formula | C28H32N4O2S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1428327-31-4 |
| PubChem ID | 66553218 |
| InChI Key | XREFXUCWSYMIOG-UHFFFAOYSA-N |
| Smiles | O=C(NCC4(CCOCC4)N3CCN(C5=CC=CC=C5)CC3)C1=CC=CN=C1SC2=CC=CC=C2 |
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 | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 24.43 | 50 | |
| DMSO | 48.86 | 100 |
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 |
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Product Datasheets for JNJ 47965567
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
4 Citations 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
Rita et al (2018) Microglial glutamate release evoked by α-synuclein aggregates is prevented by dopamine. Glia 66 2353-2365 PMID: 30394585
Andras et al (2022) Detection and Functional Evaluation of the P2X7 Receptor in hiPSC Derived Neurons and Microglia-Like Cells. Front Mol Neurosci 14 793769 PMID: 35095416
McEwan et al (2021) Autocrine regulation of wound healing by ATP release and P2Y 2 receptor activation Life Sci 283 119850 PMID: 34314735
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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Good inhibitor.
By
Stefan Uderhardt on 06/06/2020
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: phagocyte
DMSO dilution 100 μM
In vivo usage.
By
Spandita Dutta on 08/07/2018
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: Hippocampal neurons
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.
P2X7 blocker.
By
Anonymous on 01/31/2018
Assay Type: Ex Vivo
Species: Mouse
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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P2X and P2Y Receptors Scientific Review
Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.