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Submit ReviewA 967079
Description: Selective TRPA1 channel blocker
Alternative Names: A-079
Chemical Name: (1E,3E)-1-(4-Fluorophenyl)-2-methyl-1-pentene-3-one oxime
Purity: ≥98% (HPLC)
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
A 967079 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for A 967079
| M. Wt | 207.24 |
| Formula | C12H14FNO |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1170613-55-4 |
| PubChem ID | 42641861 |
| InChI Key | HKROEBDHHKMNBZ-CHBKHGQFSA-N |
| Smiles | FC1=CC=C(/C=C(C)/C(CC)=N/O)C=C1 |
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 | |
|---|---|---|---|
| Solubility | |||
| DMSO | 20.72 | 100 | |
| ethanol | 20.72 | 100 |
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 |
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Product Datasheets for A 967079
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
If you know of a relevant reference for A 967079, please let us know.
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Keywords: A 967079, A 967079 supplier, A967079, TRPA1, blockers, selective, TRP, channels, transient, receptor, potential, A-079, 4716, Tocris Bioscience
12 Citations for A 967079
Citations are publications that use Tocris products. Selected citations for A 967079 include:
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
Paulsen et al (2015) Structure of the TRPA1 ion channel suggests regulatory mechanisms. Nature 520 511 PMID: 25855297
Tong et al (2022) The Role of Transient Receptor Potential A1 and G Protein-Coupled Receptor 39 in Zinc-Mediated Acute and Chronic Itch in Mice. Front Mol Neurosci 14 768731 PMID: 35095413
Georg et al (2020) Cannabidiol (CBD): a killer for inflammatory rheumatoid arthritis synovial fibroblasts. Cell Death Dis 11 714 PMID: 32873774
Xueting et al (2020) Spinal GRPR and NPRA Contribute to Chronic Itch in a Murine Model of Allergic Contact Dermatitis. J Invest Dermatol 140 1856-1866.e7 PMID: 32032577
James H et al (2020) Cannabidiol activation of vagal afferent neurons requires TRPA1. J Neurophysiol 124 1388-1398 PMID: 32965166
Georg et al (2023) Anti-Inflammatory Effects of Cannabigerol in Rheumatoid Arthritis Synovial Fibroblasts and Peripheral Blood Mononuclear Cell Cultures Are Partly Mediated by TRPA1. Int J Mol Sci 24 PMID: 36614296
Zhao et al (2020) Irritant-evoked activation and calcium modulation of the TRPA1 receptor. Nature 585 141 PMID: 32641835
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
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
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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Blocking TRPA1 function in chronic itch.
By
Jing Feng on 01/04/2018
Assay Type: In Vivo
Species: Mouse
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.
