Selective P2X4 allosteric antagonist (IC50 = 0.54 μM). Exhibits >10-fold selectivity for human P2X4 receptors over P2X1, P2X2, P2X3, P2X5 and P2X7 receptors. Binds noncompetitively at extracellular allosteric site. Effective at human and zebrafish, but not mouse and rat P2X4 receptors.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 413.11. 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|
|1 mM||2.42 mL||12.1 mL||24.21 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 are publications that support the biological activity of the product.
Ase et al (2015) Identification and characterization of a selective allosteric antagonist of human P2X4 receptor channels Mol.Pharmacol. 87 606 PMID: 25597706
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Keywords: BX 430, BX 430 supplier, BX430, selective, allosteric, noncompetitive, antagonists, antaognism, purinergic, receptors, purinoceptors, P2X4, P2X, Receptors, 5545, Tocris Bioscience
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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.