A2764 dihydrochloride 是 TRESK (K2P18.1) 的高选择性抑制剂，对 TREK-1 和 TALK-1 有一定的抑制作用。A2764 dihydrochloride 相比基底 mTRESK 电流，对激活渠道更敏感 (IC50= 6.8 μM)。A2764 dihydrochloride 可导致细胞去极化，增加细胞的兴奋性，具有探索 TRESK 通道在偏头痛和痛觉中的作用的潜力。
货号:ajcx16436
CAS:861038-72-4
分子式:C15H21Cl3N2O
分子量：351.7
溶解度:DMSO: 41.67 mg/mL (118.48 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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[1].

[1]. Lengyel M, et al. Chemically Modified Derivatives of the Activator Compound Cloxyquin Exert Inhibitory Effect on TRESK (K2P18.1) Background Potassium Channel.Mol Pharmacol. 2019 Jun;95(6):652-660.