A selective P2X7 antagonist
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JNJ-47965567

Item No. 21895

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl]-3-pyridinecarboxamide
CAS Number
1428327-31-4
Molecular Formula
C28H32N4O2S
Formula Weight
488.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mLDMSO: 30 mg/mLDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mLEthanol: 12.5 mg/mL
λmax
251 nm
SMILES
O=C(C1=CC=CN=C1SC2=CC=CC=C2)NCC3(CCOCC3)N(CC4)CCN4C5=CC=CC=C5
InChi Code
InChI=1S/C28H32N4O2S/c33-26(25-12-7-15-29-27(25)35-24-10-5-2-6-11-24)30-22-28(13-20-34-21-14-28)32-18-16-31(17-19-32)23-8-3-1-4-9-23/h1-12,15H,13-14,16-22H2,(H,30,33)
InChi Key
XREFXUCWSYMIOG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $120

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    10 mg

    $219

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    25 mg

    $462

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    Product Description

    JNJ-47965567 is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel. Activation of P2X receptors by BzATP (Item No. 15577) induces calcium flux, which is reduced by JNJ-47965567 in 1321N1 cells transfected with recombinant P2X7 human, macaque, dog, rat, or mouse protein with pIC50s of 8.3, 8.6, 8.5, 7.2, or 7.5, respectively.1 JNJ-47965567 suppresses neonatal hypoxia-induced seizures in mice and has some anticonvulsant properties in rats.2,3 It also reduces spontaneous seizures in epileptic mice even after treatment is stopped.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bhattacharya, A., Wang, Q., Ao, H., et al. Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567. Br. J. Pharmacol. 170(3), 624-640 (2013).

    2. Rodriguez-Alvarez, N., Jimenez-Mateos, E.M., Engel, T., et al. Effects of P2X7 receptor antagonists on hypoxia-induced neonatal seizures in mice. Neuropharmacology 116(2017), 351-363 (2017).

    3. Fischer, W.H., Franke, H., Krügel, U., et al. Critical evaluation of P2X7 receptor antagonists in selected seizure models. PLoS One 11(6), e0156468 (2016).

    4. Jimenez-Pacheco, A., Diaz-Hernandez, M., Arribas-Blázquez, M., et al. Transient P2X7 receptor antagonism produces lasting reductions in spontaneous seizures and gliosis in experimental temporal lobe epilepsy. J. Neurosci. 36(22), 5920-5932 (2016).