货号 | 11923-5mg |
描述 | 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.4,2,5,6 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 |
供应商 | Cayman |
应用文献 | |
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. Proceedings of the National Academy of Sciences of the United States of America 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. Molecular 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. Journal of Pharmacological and Toxicological Methods (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). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 355.4 |
分子式 | C18H21N5O3 |
CAS号 | 349085-38-7 |
稳定性 | ≥ 2 years |
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