Catalog Number: 5299
Chemical Name: 2-(Phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl-3-pyridinecarboxamide
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.
Technical Data
  • M.Wt:
    488.64
  • Formula:
    C28H32N4O2S
  • Solubility:
    Soluble to 50 mM in 1eq. HCl and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    1428327-31-4
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.
Background References
  1. Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567.
    Bhattacharya et al.
    Br.J.Pharmacol., 2013;170:624
  2. Synthesis and pharmacological characterization of two novel, brain penetrating P2X7 antagonists.
    Letavic et al.
    ACS Med.Chem.Lett., 2013;12:419

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