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Submit ReviewA 967079
说明： Selective TRPA1 channel blocker
别名： A-079
化学名： (1E,3E)-1-(4-Fluorophenyl)-2-methyl-1-pentene-3-one oxime
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for A 967079
A 967079 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for A 967079
| 分子量 | 207.24 |
| 公式 | C12H14FNO |
| 储存 | Store at +4°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for A 967079
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 20.72 | 100 | |
| ethanol | 20.72 | 100 |
制备储备液 for A 967079
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for A 967079
参考文献 for A 967079
参考文献是支持产品生物活性的出版物。
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.
按产品操作查看相关产品
关键词: A 967079, A 967079 supplier, A967079, TRPA1, blockers, selective, TRP, channels, transient, receptor, potential, A-079, 4716, Tocris Bioscience
12 篇 A 967079 的引用文献
引用文献是使用了 Tocris 产品的出版物。 A 967079 的部分引用包括：
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
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
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A 967079 的评论
平均评分: 5 (Based on 1 Review.)
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Blocking TRPA1 function in chronic itch.
By
Jing Feng on 01/04/2018
分析类型： In Vivo
种属： 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.
