Selective TRPA1 channel blocker (IC50 values are 67 and 289 nM at human and rat TRPA1 receptors respectively). Displays 1000-fold selectivity for TRPA1 over other TRP channels, and is >150-fold selective over 75 other ion channels, enzymes and G-protein-coupled receptors. Exhibits analgesic effects in a rat osteoarthritic pain model.
|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 207.24. 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||4.83 mL||24.13 mL||48.25 mL|
|5 mM||0.97 mL||4.83 mL||9.65 mL|
|10 mM||0.48 mL||2.41 mL||4.83 mL|
|50 mM||0.1 mL||0.48 mL||0.97 mL|
References are publications that support the biological activity of the product.
McGaraughty et al (2010) TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats. Mol.Pain 6 14 PMID: 20205719
Chen et al (2011) Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation. Pain 152 1165 PMID: 21402443
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Keywords: A 967079, A 967079 supplier, A967079, TRPA1, blockers, selective, TRP, channels, transient, receptor, potential, 4716, Tocris Bioscience
2 Citations for A 967079
Citations are publications that use Tocris products. Selected citations for A 967079 include:
Paulsen et al (2015) Structure of the TRPA1 ion channel suggests regulatory mechanisms. Nature 520 511 PMID: 25855297
Ganley et al (2015) Inhibitory Interneurons That Express GFP in the PrP-GFP Mouse Spinal Cord Are Morphologically Heterogeneous, Innervated by Several Classes of Primary Afferent and Include Lamina I Projection Neurons among Their Postsynaptic Targets. Mol Brain 35 7626 PMID: 25972186
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Reviews for A 967079
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A967079 was used in the animal behavior test to block the TRPA1-mediated chronic itch at the concentration of 10mg/Kg
It may be a little difficult to dissolve the drug at a higher concentration.
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.