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Biological Activity for A 839977
A 839977 is a potent P2X7 antagonist; blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM respectively). Displays antinociceptive effects in rat and mice models of inflammatory pain. CNS penetrant.
Technical Data for A 839977
|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.
Solubility Data for A 839977
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for A 839977
The following data is based on the product molecular weight 413.26. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.42 mL||12.1 mL||24.2 mL|
|5 mM||0.48 mL||2.42 mL||4.84 mL|
|10 mM||0.24 mL||1.21 mL||2.42 mL|
|50 mM||0.05 mL||0.24 mL||0.48 mL|
References for A 839977
References are publications that support the biological activity of the product.
Honore et al (2009) The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1αβ knockout mice. Behav.Brain.Res. 204 77 PMID: 19464323
Friedle et al (2010) Recent patents on novel P2X7 receptor antagonists and their potential for reducing central nervous system inflammation. Recent Pat.CNS Drug Discov. 5 35 PMID: 19705995
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Keywords: A 839977, A 839977 supplier, A839977, purinergics, purinoceptors, purines, p2x7, antagonists, antinociceptive, cns, penetrant, P2X, Receptors, 4232, Tocris Bioscience
1 Citation for A 839977
Citations are publications that use Tocris products. Selected citations for A 839977 include:
Gangadharan et al (2015) Caveolin-1 regulates P2X7 receptor signaling in osteoblasts. PLoS One 308 C41 PMID: 25318104
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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.