Home / P2X Receptor Antagonists / AZ 11645373

AZ 11645373

Catalog #: 3317
7 Citations Datasheet / COA / SDS
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3317/10
3317/50
AZ 11645373 | CAS No. 227088-94-0 | P2X Receptor Antagonists
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Description: Potent and selective human P2X7 antagonist

Chemical Name: 3-[1-[[(3'-Nitro[1,1'-biphenyl]-4-yl)oxy]methyl]-3-(4-pyridinyl)propyl]-2,4-thiazolidinedione

Purity: ≥98%

Product Details
Citations (7)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

AZ 11645373 is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from AstraZeneca

Background References

  1. C3a modulates IL-1beta secretion in human monocytes by regulating ATP efflux and subsequent NLRP3 inflammasome activation.
    Asgari E, Le Friec G, Yamamoto H, Perucha E, Sacks S, Kohl J, Cook H, Kemper C
    Blood, 2013;122(20):3473-81.
  2. The ATP Receptors P2X7 and P2X4 Modulate High Glucose and Palmitate-Induced Inflammatory Responses in Endothelial Cells.
    Sathanoori R, Sward K, Olde B, Erlinge D
    PLoS ONE, 2015;10(5):e0125111.
  3. The P2X7 receptor is an upstream regulator of dynamic blebbing and a pluripotency marker in human embryonic stem cells
    NJ Weng, P Talbot
    Stem Cell Res, 2017;23(0):39-49.
  4. Characterization of a selective and potent antagonist of human P2X7 receptors, AZ11645373.
    Stokes et al.
    Br.J.Pharmacol., 2006;149:880
  5. Mechanism of action of species-selective P2X(7) receptor antagonists.
    Michel et al.
    Br.J.Pharmacol., 2009;156:1312
  6. Novel P2X7 receptor antagonists.
    Alcaraz et al.
    Bioorg.Med.Chem.Letts., 2003;13:4043

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Citations for AZ 11645373

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

7 Citations: Showing 1 - 7

  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. The ATP Receptors P2X7 and P2X4 Modulate High Glucose and Palmitate-Induced Inflammatory Responses in Endothelial Cells.
    Authors: Sathanoori Et al.
    PLoS One  2015;10:e0125111
  5. An Improved Method for P2X7R Antagonist Screening.
    Authors: Soares-Bezerra Et al.
    Arthritis Rheumatol  2015;10:e0123089
  6. Probenecid blocks human P2X7 receptor-induced dye uptake via a pannexin-1 independent mechanism.
    Authors: Bhaskaracharya Et al.
    PLoS One  2014;9:e93058
  7. 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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