HC030031 化学特性,用途語,生産方法
外観
白色～ほとんど白色, 結晶性粉末～粉末
溶解性
DMSOに可溶
説明
Transient receptor potential cation channel A
1 (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. HC-
030031 is a selective TRPA1 blocker, antagonizing TRPA1-
mediated calcium influx induced by AITC and formalin (IC
50s = 6.2 and 5.3 μM, respectively). It does not block currents mediated by TRPV1, TRPV3, TRPV4 hERG, or Na
V1.2 channels. HC-
030031 can be used in cells or delivered to animals orally, by inhalation, or by injection. 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.
化学的特性
White Solid
使用
A TRPA1 (transient receptor potential) selective antagonist, attenuates inflammatory- and neuropathy-induced mechanical hypersensitivity.
生物活性
Selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx (IC 50 values are 6.2 and 5.3 μ M respectively). Does not block currents mediated by TRPV1, TRPV3, TRPV4, hERG or Na V 1.2 channels. Inhibits AITC- and formalin-induced flinching in vivo .
HC030031 上流と下流の製品情報
原材料
準備製品