Биологическая активность
A2764 dihydrochloride is a highly селективный ингибитор 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 клетка depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception.
Оригинал на английском
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.
Химические свойства
- CAS №
- 861038-72-4
- Брутто-формула
- C₁₅H₂₁Cl₃N₂O
- Мол. масса
- 351.69 г/моль
- SMILES
- ClC1C=CC(OCCN(CC)CC)=C2C=1C=CC=N2.[H]Cl.[H]Cl
- Синонимы
- A2764; A-2764; A 2764
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО Publication: [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.
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.