JNJ 47965567

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Cat.No. 5299 - JNJ 47965567 | C28H32N4O2S | CAS No. 1428327-31-4
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)
Datasheet
Citations
Literature

Biological Activity

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

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Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. HCl 24.43 50
DMSO 48.86 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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: JNJ47965567 potent selective p2x7 purinergics antagonists brain penetrant P2X Receptors

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