HC 030031

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Cat.No. 2896 - HC 030031 | C18H21N5O3 | CAS No. 349085-38-7
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)
Datasheet
Citations (13)
Literature

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
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.54 100
ethanol 1.78 5

Preparing Stock Solutions

The following data is based on the product molecular weight 355.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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:


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Keywords: HC 030031, supplier, Selective, TRPA1, blockers, Channels, Transient, Receptor, Potential, HC030031, TRPA1, TRPA1, Tocris Bioscience

13 Citations for HC 030031

Citations are publications that use Tocris products. Selected citations for HC 030031 include:

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

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

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

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

Bodkin et al (2014) Investigating the potential role of TRPA1 in locomotion and cardiovascular control during hypertension. Pharmacol Res Perspect 2 e00052 PMID: 25505598

Aubdool et al (2014) TRPA1 is essential for the vascular response to environmental cold exposure. J Zhejiang Univ Sci B 5 5732 PMID: 25501034

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

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

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

Kunkler et al (2011) TRPA1 receptors mediate environmental irritant-induced meningeal vasodilatation. Pain 152 38 PMID: 21075522


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Literature in this Area

Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
Pain

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.

Pathways for HC 030031

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