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).
Sold for research purposes under agreement from AstraZeneca
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 463.51. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.1 mM||21.57 mL||107.87 mL||215.75 mL|
|0.5 mM||4.31 mL||21.57 mL||43.15 mL|
|1 mM||2.16 mL||10.79 mL||21.57 mL|
|5 mM||0.43 mL||2.16 mL||4.31 mL|
References are publications that support the biological activity of the product.
Stokes et al (2006) Characterization of a selective and potent antagonist of human P2X7 receptors, AZ11645373. Br.J.Pharmacol. 149 880 PMID: 17031385
Michel et al (2009) Mechanism of action of species-selective P2X(7) receptor antagonists. Br.J.Pharmacol. 156 1312 PMID: 19309360
Alcaraz et al (2003) Novel P2X7 receptor antagonists. Bioorg.Med.Chem.Letts. 13 4043
If you know of a relevant reference for AZ 11645373, please let us know.
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Keywords: AZ 11645373, AZ 11645373 supplier, Potent, selective, human, P2X7, antagonists, Receptors, Purinergic, purinoceptors, AZ11645373, AstraZeneca, P2X, 3317, Tocris Bioscience
7 Citations for AZ 11645373
Citations are publications that use Tocris products. Selected citations for AZ 11645373 include:
Sathanoori et al (2015) The ATP Receptors P2X7 and P2X4 Modulate High Glucose and Palmitate-Induced Inflammatory Responses in Endothelial Cells. PLoS One 10 e0125111 PMID: 25938443
Kawano et al (2015) Autocrine Regulation of UVA-Induced IL-6 Production via Release of ATP and Activation of P2Y Receptors. PLoS One 10 e0127919 PMID: 26030257
Karmakar et al (2016) Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP. Nat.Commun. 7 10555 PMID: 26877061
Soares-Bezerra et al (2015) An Improved Method for P2X7R Antagonist Screening. Arthritis Rheumatol 10 e0123089 PMID: 25993132
Bhaskaracharya et al (2014) Probenecid blocks human P2X7 receptor-induced dye uptake via a pannexin-1 independent mechanism. PLoS One 9 e93058 PMID: 24671093
Agrawal et al (2016) P2X7Rs are involved in cell death, growth and cellular signaling in primary human osteoblasts Bone 95 91 PMID: 27856358
Foster et al (2013) Mitochondrial superoxide generation enhances P2X7R-mediated loss of cell surface CD62L on naive human CD4+ T lymphocytes. J Immunol 190 1551 PMID: 23319734
Do you know of a great paper that uses AZ 11645373 from Tocris? Please let us know.
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Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.