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Biological Activity for A 967079
A 967079 (also known as A-079) is a selective TRPA1 channel blocker (IC50 values are 67 and 289 nM at human and rat TRPA1 receptors respectively) that 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. A 967079 exhibits analgesic effects in a rat osteoarthritic pain model.
External Portal Information for A 967079
The Chemical Probes pages of the Structural Genomics Consortium website are a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of A 967079 (A-079) is reviewed.
Compound Libraries for A 967079
Technical Data for A 967079
|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 967079
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for A 967079
The following data is based on the product molecular weight 207.24. 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||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 for A 967079
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, A-079, 4716, Tocris Bioscience
7 Citations for A 967079
Citations are publications that use Tocris products. Selected citations for A 967079 include:
Zhao et al (2020) Irritant-evoked activation and calcium modulation of the TRPA1 receptor. Nature 585 141 PMID: 32641835
Cheng et al (2019) The role of Nav1.7 and methylglyoxal-mediated activation of TRPA1 in itch and hypoalgesia in a murine model of type 1 diabetes. Theranostics 9 4287 PMID: 31285762
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
Paulsen et al (2015) Structure of the TRPA1 ion channel suggests regulatory mechanisms. Nature 520 511 PMID: 25855297
Jiang et al (2019) ROS/TRPA1/CGRP signaling mediates cortical spreading depression. J Headache Pain 20 25 PMID: 30841847
Ko et al (2019) A critical evaluation of TRPA1-mediated locomotor behavior in zebrafish as a screening tool for novel anti-nociceptive drug discovery. Sci Rep 9 2430 PMID: 30787340
Wu et al (2017) Ethyl Vanillin Activates TRPA1. J Pharmacol Exp Ther 362 368 PMID: 28620120
Do you know of a great paper that uses A 967079 from Tocris? Please let us know.
Reviews for A 967079
Average Rating: 5 (Based on 1 Review.)
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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.