HC 030031

Catalog # Availability Size / Price Qty
2896/10
2896/50
HC 030031 | CAS No. 349085-38-7 | TRPA1 Blockers
1 Image
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%

Product Details
Citations (31)
Reviews (1)

Biological Activity

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.

Technical Data

M.Wt:
355.39
Formula:
C18H21N5O3
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥99%
Storage:
Store at RT
CAS No:
349085-38-7

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.

Background References

  1. Prostaglandin-induced activation of nociceptive neurons via direct interactions with TRPA1.
    Taylor-Clark et al.
    Mol.Pharmacol., 2008;73:274
  2. TRPA1 mediates formalin-induced pain.
    McNamara et al.
    Proc.Natl.Acad.Sci.USA, 2007;104:13525

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Citations for HC 030031

The citations listed below are publications that use Tocris products. Selected citations for HC 030031 include:

31 Citations: Showing 1 - 10

  1. The role of Nav1.7 and methylglyoxal-mediated activation of TRPA1 in itch and hypoalgesia in a murine model of type 1 diabetes.
    Authors: Cheng Et al.
    Theranostics  2019;9:4287
  2. A critical evaluation of TRPA1-mediated locomotor behavior in zebrafish as a screening tool for novel anti-nociceptive drug discovery.
    Authors: Ko Et al.
    Sci Rep  2019;9:2430
  3. Bladder Dysfunction in an Obese Zucker Rat: The Role of TRPA1 Channels, Oxidative Stress, and Hydrogen Sulfide.
    Authors: Blaha Et al.
    Oxid Med Cell Longev  2019;2019:5641645
  4. Relevance of TRPA1 and TRPM8 channels as vascular sensors of cold in the cutaneous microvasculature.
    Authors: Pan Et al.
    Pflugers Arch  2018;470:779
  5. Transient Opening of the Mitochondrial Permeability Transition Pore Induces Microdomain Calcium Transients in Astrocyte Processes.
    Authors: Agarwal Et al.
    Neuron  2017;93:587
  6. TRPA1-FGFR2 binding event is a regulatory oncogenic driver modulated by miRNA-142-3p.
    Authors: Berrout Et al.
    Nat Commun  2017;8:947
  7. Methylglyoxal Requires AC1 and TRPA1 to Produce Pain and Spinal Neuron Activation.
    Authors: Griggs Et al.
    Front Neurosci  2017;11:679
  8. Modulation of breast cancer cell viability by a cannabinoid receptor 2 agonist, JWH-015, is calcium dependent.
    Authors: Hanlon Et al.
    Breast Cancer (Dove Med Press)  2016;8:59
  9. Effects of ε-viniferin, a dehydrodimer of resveratrol, on transepithelial active ion transport and ion permeability in the rat small and large intestinal mucosa.
    Authors: Karaki Et al.
    Physiol Rep  2016;4
  10. Environmental cold exposure increases blood flow and affects pain sensitivity in the knee joints of CFA-induced arthritic mice in a TRPA1-dependent manner.
    Authors: Fernandes Et al.
    Mol Pain  2016;18:7
  11. Hydrogen sulfide-induced itch requires activation of Cav3.2 T-type calcium channel in mice.
    Authors: Wang Et al.
    World J Gastroenterol  2015;5:16768
  12. Structure of the TRPA1 ion channel suggests regulatory mechanisms.
    Authors: Paulsen Et al.
    Nature  2015;520:511
  13. Alterations in serotonin, transient receptor potential channels and protease-activated receptors in rats with irritable bowel syndrome attenuated by Shugan decoction.
    Authors: Shi Et al.
    Arthritis Res Ther  2015;21:4852
  14. Antinociceptive activity of transient receptor potential channel TRPV1, TRPA1, and TRPM8 antagonists in neurogenic and neuropathic pain models in mice.
    Authors: Sałat and Filipek
    J Neurosci  2015;16:167
  15. Released lipids regulate transient receptor potential channel (TRP)-dependent oral cancer pain.
    Authors: Ruparel Et al.
    Nat Commun  2015;11:30
  16. Menthol suppresses laryngeal C-fiber hypersensitivity to cigarette smoke in a rat model of gastroesophageal reflux disease: the role of TRPM8.
    Authors: Liu Et al.
    J Appl Physiol (1985)  2015;118:635
  17. Differential Contribution of TRPA1, TRPV4 and TRPM8 to Colonic Nociception in Mice.
    Authors: Mueller-Tribbensee Et al.
    PLoS One  2015;10:e0128242
  18. TRPA1 is essential for the vascular response to environmental cold exposure.
    Authors: Aubdool Et al.
    J Zhejiang Univ Sci B  2014;5:5732
  19. Investigating the potential role of TRPA1 in locomotion and cardiovascular control during hypertension.
    Authors: Bodkin Et al.
    Pharmacol Res Perspect  2014;2:e00052
  20. Sensory nerve terminal mitochondrial dysfunction activates airway sensory nerves via transient receptor potential (TRP) channels.
    Authors: Nesuashvili Et al.
    Mol Pharmacol  2013;83:1007
  21. Hydrogen sulfide induces hypersensitivity of rat capsaicin-sensitive lung vagal neurons: role of TRPA1 receptors.
    Authors: Hsu Et al.
    Am J Physiol Regul Integr Comp Physiol  2013;305:R769
  22. The molecular basis for species-specific activation of human TRPA1 protein by protons involves poorly conserved residues within transmembrane domains 5 and 6.
    Authors: Roche Et al.
    J Biol Chem  2013;288:20280
  23. Activation of TRPA1 by luminal stimuli induces EP4-mediated anion secretion in human and rat colon.
    Authors: Kaji Et al.
    Am J Physiol Gastrointest Liver Physiol  2012;302:G690
  24. Oxidative stress induces itch via activation of transient receptor potential subtype ankyrin 1 in mice.
    Authors: Liu and Ji
    Neurosci Bull  2012;28:145
  25. Involvement of the endogenous hydrogen sulfide/Ca(v) 3.2 T-type Ca2+ channel pathway in cystitis-related bladder pain in mice.
    Authors: Matsunami Et al.
    Br J Pharmacol  2012;167:917
  26. Inhibitory effect of cannabichromene, a major non-psychotropic cannabinoid extracted from Cannabis sativa, on inflammation-induced hypermotility in mice.
    Authors: Izzo Et al.
    Br J Pharmacol  2012;166:1444
  27. Modulation of mouse gastrointestinal motility by allyl isothiocyanate, a constituent of cruciferous vegetables (Brassicaceae): evidence for TRPA1-independent effects.
    Authors: Capasso Et al.
    Br J Pharmacol  2012;165:1966
  28. Spinal 12-lipoxygenase-derived hepoxilin A3 contributes to inflammatory hyperalgesia via activation of TRPV1 and TRPA1 receptors.
    Authors: Gregus Et al.
    Proc Natl Acad Sci U S A  2012;109:6721
  29. Ocular dryness excites two classes of corneal afferent neurons implicated in basal tearing in rats: involvement of transient receptor potential channels.
    Authors: Hirata
    J Neurophysiol  2012;107:1199
  30. Effects of luminal thymol on epithelial transport in human and rat colon.
    Authors: Kaji Et al.
    Am J Physiol Gastrointest Liver Physiol  2011;300:G1132
  31. TRPA1 receptors mediate environmental irritant-induced meningeal vasodilatation.
    Authors: Kunkler Et al.
    Pain  2011;152:38

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blocking dTRPA1 in fruit fly embryos
By Ginger Hunter on 01/04/2018
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.


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