| Bioactivity | A2793 is an efficient dual TWIK-related acid-sensitive K+ channel (TASK)-1/TRESK inhibitor, with an IC50 of 6.8 μM for mTRESK. A2764 is more selective for TRESK, and it only moderately influences TREK-1 and TALK-1[1]. | |||||||||
| Target | IC50: 6.8 μM (mTRESK). | |||||||||
| Invitro | A2793 (100 µM) inhibits the unstimulated channel by 43.0±8.9% (n=5) while after ionomycin activation the reduction of the TRESK current is 85.5±2.9% (n=5)[1].A2793 inhibits TASK-1 (100 µM, 53.4±13,5%, n=5), while A2764 is more selective for TRESK, it only moderately influencesTREK-1 and TALK-1[1].A2793 may be considered as a tool to discriminate between the resting and activated channels in heterologous expression systems, and to block TRESK activated by calcineurin in the native cells which do not express TASK-1[1]. | |||||||||
| Name | A2793 | |||||||||
| CAS | 88349-90-0 | |||||||||
| Formula | C13H12ClNO3 | |||||||||
| Molar Mass | 265.69 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Miklós Lengyel, et al. Chemically Modified Derivatives of the Activator Compound Cloxyquin Exert Inhibitory Effect on TRESK (K 2P 18.1) Background Potassium Channel. Mol Pharmacol. 2019 Jun;95(6):652-660. |