TRPA1
TRPA1 is a calcium-permeable, non-selective cation channel expressed mainly in nociceptive sensory neurons, where it detects harmful chemical stimuli and amplifies pain transmission[1][2]. Mechanistically, TRPA1 activation drives Ca2+ influx, neuropeptide release, neurogenic inflammation, and hypersensitivity to mechanical or cold stimuli[2][3]. In disease models, TRPA1 contributes to inflammatory pain, diabetic neuropathy, aromatase inhibitor-evoked pain, itch, migraine-related CGRP release, and airway inflammation models[1][4][5][6][7]. Compared with related isoforms, TRPA1 responds broadly to reactive oxidative, nitrative, and carbonyl stress products, while TRPV1 and TRPV4 represent functionally related but distinct TRP channels in pain and inflammation studies[3][8]. For experimental applications, AITC and JT010 activate TRPA1, whereas HC-030031, A967079, TCS 5861528, pinosylvin, and dual TRPV4/TRPA1 inhibitors support mechanistic studies of TRPA1-dependent calcium influx, cytokine production, edema, and pain behavior[6][7][8][9].
References:
- [1]. Koivisto A, et al. TRPA1 Antagonists for Pain Relief. Pharmaceuticals (Basel). 2018 Nov 1;11(4):117. [Content Brief]
- [2]. Bautista DM, et al. TRPA1: A gatekeeper for inflammation. Annu Rev Physiol. 2013;75:181-200. [Content Brief]
- [3]. Iannone LF, et al. Neuronal and non-neuronal TRPA1 as therapeutic targets for pain and headache relief. Temperature (Austin). 2022 May 29;10(1):50-66. [Content Brief]
- [4]. De Logu F, et al. TRPA1 Mediates Aromatase Inhibitor-Evoked Pain by the Aromatase Substrate Androstenedione. Cancer Res. 2016 Dec 1;76(23):7024-7035. [Content Brief]
- [5]. Cevikbas F, et al. A sensory neuron-expressed IL-31 receptor mediates T helper cell-dependent itch: Involvement of TRPV1 and TRPA1. J Allergy Clin Immunol. 2014 Feb;133(2):448-60. [Content Brief]
- [6]. Belinskaia M, et al. Bipartite Activation of Sensory Neurons by a TRPA1 Agonist Allyl Isothiocyanate Is Reflected by Complex Ca2+ Influx and CGRP Release Patterns: Enhancement by NGF and Inhibition with VAMP and SNAP-25 Cleaving Botulinum Neurotoxins. Int J Mol Sci. 2023 Jan 10;24(2):1338. [Content Brief]
- [7]. Singh U, et al. Investigation of the Pathomechanism of Chronic Cough Using an In Vitro Approach. Clin Exp Allergy. 2025 Mar;55(3):247-249. [Content Brief]
- [8]. Kanju P, et al. Small molecule dual-inhibitors of TRPV4 and TRPA1 for attenuation of inflammation and pain. Sci Rep. 2016 Jun 1;6:26894. [Content Brief]
- [9]. Moilanen LJ, et al. Pinosylvin Inhibits TRPA1-Induced Calcium Influx In Vitro and TRPA1-Mediated Acute Paw Inflammation In Vivo. Basic Clin Pharmacol Toxicol. 2016 Mar;118(3):238-42. [Content Brief]
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TRPA1 Related Products (33)
Related Products (33)
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TRPV1-IN-2
0 ImagesCat. No.: HY-162856TRPV1-IN-2 ((R)-32) is a TRPV1 inhibitor. TRPV1-IN-2 has protective effects on ED epilepsy models.
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Neoambrosin
0 ImagesCat. No.: HY-127003CAS No.: 18446-70-3Neoambrosin is a sesquiterpene lactone. Neoambrosin acts as a partial agonist of PPARγ and TRPA1 receptors, with no carbonic anhydrase inhibitory activity. Neoambrosin can be used in research on hypoglycemia, analgesia, anti-inflammation and anticancer effects.
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Artepillin C (Standard)
0 ImagesCat. No.: HY-N10319RCAS No.: 72944-19-5Artepillin C (Standard) is the analytical standard of Artepillin C (HY-N10319). This product is intended for research and analytical applications. Artepillin C is an orally active CREB/CRTC2 inhibitor and TRPA1 covalent agonist (EC50=1.8 μM). Artepillin C inhibits CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression to regulate glucose and lipid metabolism. Artepillin C can also activate TRPA1 channels to induce spicy taste signals. Artepillin C can inhibit tumor cell proliferation, induce apoptosis, improve insulin resistance and inhibit liver lipid synthesis. Artepillin C can be used in the study of metabolic syndrome, tumor prevention and treatment, and inflammation.
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ZQMT-10
0 ImagesCat. No.: HY-170652CAS No.: 1791309-86-8
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Cannabitwinol
0 ImagesCat. No.: HY-179432CAS No.: 2699950-81-5Synonyms: CBDDCannabitwinol is a selective thermosensitive TRP modulator and NF-κB inhibitor. Cannabitwinol inhibits TNFα-induced NF-κB-driven transcription and TNFα-induced IL-8 release, and exhibits anti-inflammatory and antioxidant activities. Cannabitwinol shows selectivity for cold-activated TRP channels, activating TRPA1 (EC50 = 3.0 μM) and antagonizing TRPM8 (IC50 = 3.9 μM), but has no significant affinity for heat-activated TRP channels such as TRPV1 and TRPV2. Cannabitwinol can be used in research related to inflammatory skin diseases, cold allodynia, and hyperalgesia.
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AMG8788
0 ImagesCat. No.: HY-104061CAS No.: 1159996-43-6AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM.
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TRPA1-IN-5
0 ImagesCat. No.: HY-187167CAS No.: 3136943-00-2
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8,9-Epoxyeicosatrienoic acid
0 ImagesCat. No.: HY-113488CAS No.: 81246-85-78,9-Epoxyeicosatrienoic acid has an unique protective effect on glomeruli. 8,9-Epoxyeicosatrienoic acid blocks the increase in glomerular albumin permeability caused by circulating permeability factor (FSPF). 8,9-Epoxyeicosatrienoic acid can be used for the research of glomerular dysfunction.
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AMG9678
0 ImagesCat. No.: HY-104062CAS No.: 1159997-27-9AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM.
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TRPV4/TRPA1-IN-1
0 ImagesCat. No.: HY-122692CAS No.: 1532515-60-8TRPV4/TRPA1-IN-1 is a TRPV4/TRPA1 inhibitor that suppresses TRPV4/TRPA1-mediated calcium influx. TRPV4/TRPA1-IN-1 alleviates pain behaviors in a mouse trigeminal stimulation pain model and inhibits inflammation and pain-related behaviors in a mouse acute pancreatitis model. TRPV4/TRPA1-IN-1 can be used in research on acute pancreatitis.
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GRC-17536
0 ImagesCat. No.: HY-187618CAS No.: 1508276-29-6GRC-17536 is a TRPA1 antagonist with selective inhibition of TRPA1-mediated calcium influx.GRC-17536 binds to TRPA1 binding site 2 to inhibit channel activity.GRC-17536 reduces irritant-induced cough responses and citric acid-induced cough responses.GRC-17536 exhibits antitussive activity.GRC-17536 has poor pharmacokinetic and bioavailability properties, leading to discontinued development after a Phase IIa study.GRC-17536 can be used for the research of painful diabetic polyneuropathy, peripheral diabetic neuropathy, asthma, and chronic cough.
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Carvacryl acetate
0 ImagesCarvacryl acetate is an orally active and brain-penetrant TRPA1 receptor activator and Na+/K+-ATPase activator. Carvacryl acetate modulates GABAergic signaling, alters hippocampal GABA and glutamine levels, reduces lipid peroxidation and nitrite formation, scavenges hydroxyl radicals, and boosts glutathione and antioxidant enzyme activity. Carvacryl acetate inhibits Haemonchus contortus larval hatching, development, adult motility, and fecal egg counts, and induces adult worm structural damage. Carvacryl acetate can be used for the research of intestinal mucositis, gastrointestinal nematode infection, epilepsy, and neurodegenerative diseases.
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TRPA1-IN-3
0 ImagesTRPA1-IN-3 (commound 1) is a TRPA1 inhibitor. TRPA1-IN-3 can be used in skin and respiratory tract related research.
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