Molecular Formula | C13H12ClNO3 |
Molar Mass | 265.69 |
Density | 1.291±0.06 g/cm3(Predicted) |
Boling Point | 393.4±27.0 °C(Predicted) |
Solubility | Soluble in DMSO |
pKa | 1.97±0.29(Predicted) |
Storage Condition | -20℃ |
Use | 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 |
In vitro study | 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). A2793 inhibits TASK-1 (100 µM, 53.4±13,5%, n=5), while A2764 is more selective for TRESK, it only moderately influences TREK-1 and TALK-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. |
Reference Show more | [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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 0 ml | 0 ml | 0 ml |
5 mM | 0 ml | 0 ml | 0 ml |
10 mM | 0 ml | 0 ml | 0 ml |
5 mM | 0 ml | 0 ml | 0 ml |
biological activity | A2793 (Ethyl [(5-Chloroquinolin-8-yl)oxy]acetate) is TWIK-related spinal cord potential channel (TRESK, k2P18, KCNK18) and TASK-1 (KCNK3), The IC50 value for mouse TRESK was 6.8 μm. |
Target | Value |
mTRESK (Cell-free assay) | 6.8 μM |