Selective TRPA1 channel blocker
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Isomer(s)
19310AZ 7371
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HC-030031

Item No. 11923

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,2,3,6-tetrahydro-1,3-dimethyl-N-[4-(1-methylethyl)phenyl]-2,6-dioxo-7H-purine-7-acetamide
CAS Number
349085-38-7
Molecular Formula
C18H21N5O3
Formula Weight
355.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 10 mg/ml
λmax
248 nm
SMILES
CN(C(C(N(CC(NC1=CC=C(C(C)C)C=C1)=O)C=N2)=C2N3C)=O)C3=O
InChi Code
InChI=1S/C18H21N5O3/c1-11(2)12-5-7-13(8-6-12)20-14(24)9-23-10-19-16-15(23)17(25)22(4)18(26)21(16)3/h5-8,10-11H,9H2,1-4H3,(H,20,24)
InChi Key
HEQDZPHDVAOBLN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $31

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    10 mg

    $53

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    50 mg

    $154

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    Product Description

    Transient receptor potential cation channel A1 (TRPA1) is an ankyrin-like ion channel which acts as a sensor for chemical irritants, pain, and cold. It is activated by allyl isothiocyanate (AITC), formalin, hydrogen peroxide, tear gas, and other compounds.1,2,3 HC-030031 is a selective TRPA1 blocker, antagonizing TRPA1-mediated calcium influx induced by AITC and formalin (IC50s = 6.2 and 5.3 μM, respectively).2 It does not block currents mediated by TRPV1, TRPV3, TRPV4 hERG, or NaV1.2 channels.2 HC-030031 can be used in cells or delivered to animals orally, by inhalation, or by injection.2,4,5,6 Oral administration (100 mg/kg) of HC-030031 significantly reversed mechanical hypersensitivity in rat models of chronic inflammatory or neuropathic pain, while local injection (100 μg) into inflamed mouse hind paws attenuated mechanical, but not heat, hypersensitivity.4,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Macpherson, L.J., Dubin, A.E., Evans, M.J., et al. Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines. Nature 445(7127), 541-545 (2007).

    2. McNamara, C.R., Mandel-Brehm, J., Bautista, D.M., et al. TRPA1 mediates formalin-induced pain. Proc. Natl. Acad. Sci. USA 104(33), 13525-13530 (2007).

    3. Andrade, E.L., Luiz, A.P., Ferreira, J., et al. Pronociceptive response elicited by TRPA1 receptor activation in mice. Neuroscience 152(2), 511-520 (2008).

    4. Eid, S.R., Crown, E.D., Moore, E.L., et al. HC-030031, a TRPAI selective antagonist, attenuates inflammatory- and neuropathy-induced mechanical hypersensitivity. Mol. Pain 4(48), (2008).

    5. Daller, J.R., Wong, J., Brooks, B.D., et al. An inexpensive system for evaluating the tussive and anti-tussive properties of chemicals in conscious, unrestrained guinea pigs. J. Pharmacol. Toxicol. Methods 66(3), 232-237 (2012).

    6. Lennertz, R.C., Kossyreva, E.A., Smith, A.K., et al. TRPA1 mediates mechanical sensitization in nociceptors during inflammation. PLoS One 7(8), (2012).