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Submit ReviewHC 030031
Description: Selective TRPA1 blocker
Chemical Name: 2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(4-isopropylphenyl)acetamide
Purity: ≥99% (HPLC)
Biological Activity for HC 030031
HC 030031 is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx (IC50 values are 6.2 and 5.3 μM respectively). Does not block currents mediated by TRPV1, TRPV3, TRPV4, hERG or NaV1.2 channels. Inhibits AITC- and formalin-induced flinching in vivo.
Compound Libraries for HC 030031
HC 030031 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for HC 030031
| M. Wt | 355.39 |
| Formula | C18H21N5O3 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 349085-38-7 |
| PubChem ID | 1150897 |
| InChI Key | HEQDZPHDVAOBLN-UHFFFAOYSA-N |
| Smiles | O=C1C2=C(N=CN2CC(NC3=CC=C(C(C)C)C=C3)=O)N(C)C(N1C)=O |
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 HC 030031
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.54 | 100 |
Preparing Stock Solutions for HC 030031
The following data is based on the product molecular weight 355.39. 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 | 2.81 mL | 14.07 mL | 28.14 mL |
| 5 mM | 0.56 mL | 2.81 mL | 5.63 mL |
| 10 mM | 0.28 mL | 1.41 mL | 2.81 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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Product Datasheets for HC 030031
References for HC 030031
References are publications that support the biological activity of the product.
Taylor-Clark et al (2008) Prostaglandin-induced activation of nociceptive neurons via direct interactions with TRPA1. Mol.Pharmacol. 73 274 PMID: 18000030
McNamara et al (2007) TRPA1 mediates formalin-induced pain. Proc.Natl.Acad.Sci.USA 104 13525 PMID: 17686976
If you know of a relevant reference for HC 030031, please let us know.
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Keywords: HC 030031, HC 030031 supplier, Selective, TRPA1, blockers, Channels, Transient, Receptor, Potential, HC030031, 2896, Tocris Bioscience
31 Citations for HC 030031
Citations are publications that use Tocris products. Selected citations for HC 030031 include:
Blaha et al (2019) Bladder Dysfunction in an Obese Zucker Rat: The Role of TRPA1 Channels, Oxidative Stress, and Hydrogen Sulfide. Oxid Med Cell Longev 2019 5641645 PMID: 31531184
Karaki et al (2016) Effects of ε-viniferin, a dehydrodimer of resveratrol, on transepithelial active ion transport and ion permeability in the rat small and large intestinal mucosa. Physiol Rep 4 PMID: 27162263
Gregus et al (2012) Spinal 12-lipoxygenase-derived hepoxilin A3 contributes to inflammatory hyperalgesia via activation of TRPV1 and TRPA1 receptors. Proc Natl Acad Sci U S A 109 6721 PMID: 22493235
Izzo et al (2012) Inhibitory effect of cannabichromene, a major non-psychotropic cannabinoid extracted from Cannabis sativa, on inflammation-induced hypermotility in mice. Br J Pharmacol 166 1444 PMID: 22300105
Hirata (2012) Ocular dryness excites two classes of corneal afferent neurons implicated in basal tearing in rats: involvement of transient receptor potential channels. J Neurophysiol 107 1199 PMID: 22114162
Pan et al (2018) Relevance of TRPA1 and TRPM8 channels as vascular sensors of cold in the cutaneous microvasculature. Pflugers Arch 470 779 PMID: 29164310
Hanlon et al (2016) Modulation of breast cancer cell viability by a cannabinoid receptor 2 agonist, JWH-015, is calcium dependent. Breast Cancer (Dove Med Press) 8 59 PMID: 27186076
Fernandes et al (2016) Environmental cold exposure increases blood flow and affects pain sensitivity in the knee joints of CFA-induced arthritic mice in a TRPA1-dependent manner. Mol Pain 18 7 PMID: 26754745
Ruparel et al (2015) Released lipids regulate transient receptor potential channel (TRP)-dependent oral cancer pain. Nat Commun 11 30 PMID: 26007300
Wang et al (2015) Hydrogen sulfide-induced itch requires activation of Cav3.2 T-type calcium channel in mice. World J Gastroenterol 5 16768 PMID: 26602811
Shi et al (2015) Alterations in serotonin, transient receptor potential channels and protease-activated receptors in rats with irritable bowel syndrome attenuated by Shugan decoction. Arthritis Res Ther 21 4852 PMID: 25944998
Bodkin et al (2014) Investigating the potential role of TRPA1 in locomotion and cardiovascular control during hypertension. Pharmacol Res Perspect 2 e00052 PMID: 25505598
Griggs et al (2017) Methylglyoxal Requires AC1 and TRPA1 to Produce Pain and Spinal Neuron Activation. Front Neurosci 11 679 PMID: 29270106
Agarwal et al (2017) Transient Opening of the Mitochondrial Permeability Transition Pore Induces Microdomain Calcium Transients in Astrocyte Processes. Neuron 93 587 PMID: 28132831
Mueller-Tribbensee et al (2015) Differential Contribution of TRPA1, TRPV4 and TRPM8 to Colonic Nociception in Mice. PLoS One 10 e0128242 PMID: 26207981
Paulsen et al (2015) Structure of the TRPA1 ion channel suggests regulatory mechanisms. Nature 520 511 PMID: 25855297
Aubdool et al (2014) TRPA1 is essential for the vascular response to environmental cold exposure. J Zhejiang Univ Sci B 5 5732 PMID: 25501034
Kunkler et al (2011) TRPA1 receptors mediate environmental irritant-induced meningeal vasodilatation. Pain 152 38 PMID: 21075522
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
Sałat and Filipek (2015) Antinociceptive activity of transient receptor potential channel TRPV1, TRPA1, and TRPM8 antagonists in neurogenic and neuropathic pain models in mice. J Neurosci 16 167 PMID: 25743118
Liu et al (2015) Menthol suppresses laryngeal C-fiber hypersensitivity to cigarette smoke in a rat model of gastroesophageal reflux disease: the role of TRPM8. J Appl Physiol (1985) 118 635 PMID: 25539933
Kaji et al (2011) Effects of luminal thymol on epithelial transport in human and rat colon. Am J Physiol Gastrointest Liver Physiol 300 G1132 PMID: 21372164
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
Berrout et al (2017) TRPA1-FGFR2 binding event is a regulatory oncogenic driver modulated by miRNA-142-3p. Nat Commun 8 947 PMID: 29038531
Roche et al (2013) The molecular basis for species-specific activation of human TRPA1 protein by protons involves poorly conserved residues within transmembrane domains 5 and 6. J Biol Chem 288 20280 PMID: 23709225
Hsu et al (2013) Hydrogen sulfide induces hypersensitivity of rat capsaicin-sensitive lung vagal neurons: role of TRPA1 receptors. Am J Physiol Regul Integr Comp Physiol 305 R769 PMID: 23842678
Nesuashvili et al (2013) Sensory nerve terminal mitochondrial dysfunction activates airway sensory nerves via transient receptor potential (TRP) channels. Mol Pharmacol 83 1007 PMID: 23444014
Kaji et al (2012) Activation of TRPA1 by luminal stimuli induces EP4-mediated anion secretion in human and rat colon. Am J Physiol Gastrointest Liver Physiol 302 G690 PMID: 22207576
Matsunami et al (2012) Involvement of the endogenous hydrogen sulfide/Ca(v) 3.2 T-type Ca2+ channel pathway in cystitis-related bladder pain in mice. Br J Pharmacol 167 917 PMID: 22646666
Capasso et al (2012) Modulation of mouse gastrointestinal motility by allyl isothiocyanate, a constituent of cruciferous vegetables (Brassicaceae): evidence for TRPA1-independent effects. Br J Pharmacol 165 1966 PMID: 21955242
Liu and Ji (2012) Oxidative stress induces itch via activation of transient receptor potential subtype ankyrin 1 in mice. Neurosci Bull 28 145 PMID: 22466125
Do you know of a great paper that uses HC 030031 from Tocris? Please let us know.
Reviews for HC 030031
Average Rating: 4.5 (Based on 2 Reviews.)
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breast cancer cell viability by a cannabinoid receptor 2 agonist.
By
Anonymous on 03/15/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: MCF-7
We used all these compounds which were dissolved in DMSO and added to fresh culture media. Concentration reference paper PMID: 27186076
blocking dTRPA1 in fruit fly embryos.
By
Ginger Hunter on 01/04/2018
Assay Type: In Vivo
Species: Other
microinjection of the TRPA1 inhibitor HC 030031 into Drosophila melanogaster embryos. Drug appears to phenocopy aspects of the null mutant and RNAi knockdown of the TRPA1 gene in embryos fairly well.
