产品
编 号:F577694
分子式:C15H21Cl3N2O
分子量:351.7
产品类型
结构图
CAS No: 861038-72-4
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产品详情
生物活性:
A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception.
体外研究:
A2764 (100 μM) inhibits the background K+ current by 42.8±11.5% when it applies to the oocytes expressing mTRESK.A2764 (100 μM) shows an improvedinhibitory potency for activated channel with an IC50 of activated channel in ionomycin-activated mTRESK current.The subsequent application of A2764 strongly inhibits the current (77.8±3.5%).A2764 (100 μM) inhibits the current of TRESK under resting conditions and in the activated state by 42.8±11.5% and 77.8±3.5%, respectively.