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。

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 (IC 50 =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.

Solid

IC50: 6.8 μM (activated mTRESK channel)

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 improved inhibitory 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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: H₂O : ≥ 100 mg/mL (284.33 mM)DMSO : 41.67 mg/mL (118.48 mM; Need ultrasonic)