Catalog Number: 3317
Chemical Name: 3-[1-[[(3'-Nitro[1,1'-biphenyl]-4-yl)oxy]methyl]-3-(4-pyridinyl)propyl]-2,4-thiazolidinedione
Biological Activity
Potent and selective human P2X7 antagonist (KB values are 5 - 7 and > 10,000 nM at hP2X7 and rP2X7 respectively) that is completely without effect at all other P2X subtypes. Inhibits BzATP-mediated calcium influx and inhibits ATP-mediated IL-1β release in vitro (KB values are 15 and 92 nM respectively).
Technical Data
  • M.Wt:
    463.51
  • Formula:
    C24H21N3O5S
  • Solubility:
    Soluble to 10 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    227088-94-0
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from AstraZeneca
Background References
  1. Characterization of a selective and potent antagonist of human P2X7 receptors, AZ11645373.
    Stokes et al.
    Br.J.Pharmacol., 2006;149:880
  2. Mechanism of action of species-selective P2X(7) receptor antagonists.
    Michel et al.
    Br.J.Pharmacol., 2009;156:1312
  3. Novel P2X7 receptor antagonists.
    Alcaraz et al.
    Bioorg.Med.Chem.Letts., 2003;13:4043
Citations:

The citations listed below are publications that use Tocris products. Selected citations for AZ 11645373 include:

5 Citations: Showing 1 - 5
Filter your results:

  1. P2X7Rs are involved in cell death, growth and cellular signaling in primary human osteoblasts
    Authors: Agrawal Et al.
    Bone 2016;95:91
  2. Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP.
    Authors: Karmakar Et al.
    Nat.Commun. 2016;7:10555
  3. Autocrine Regulation of UVA-Induced IL-6 Production via Release of ATP and Activation of P2Y Receptors.
    Authors: Kawano Et al.
    PLoS One 2015;10:e0127919
  4. An Improved Method for P2X7R Antagonist Screening.
    Authors: Soares-Bezerra Et al.
    Arthritis Rheumatol 2015;10:e0123089
  5. Mitochondrial superoxide generation enhances P2X7R-mediated loss of cell surface CD62L on naive human CD4+ T lymphocytes.
    Authors: Foster Et al.
    J Immunol 2013;190:1551

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