| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
A2793 inhibited TWIK-related acid-sensitive K+ channel (TASK)-1 (100 µM, 53.4% ± 13, 5%, n = 5). The inhibitor analogs (A2764 and A2793) exerted state-dependent effects.
| Targets |
A2793 targets TRESK (K₂P18.1) background potassium channel as an inhibitor, with an IC₅₀ value of 1.8 μM (whole-cell patch-clamp assay) [1]
|
|---|---|
| ln Vitro |
When ionomycin is used to activate TRESK current, it decreases it by 85.5±2.9% (n=5), whereas A2793 (100 µM) inhibits unstimulated channels by 43.0±8.9% (n=5) [1]. While A2764 is more selective for TRESK, having only mild effects on TALK-1 and TREK-1, A2793 inhibits TASK-1 (100 µM, 53.4±13.5%, n=5) [1]. A2793 can be used as a tool in heterologous expression systems to discriminate between quiescent and activated channels and to block calcineurin-activated TRESK in native cells lacking TASK-1 expression [1].
A2793 (0.1–10 μM) dose-dependently inhibited TRESK channel currents in HEK293 cells stably expressing human TRESK, achieving 92% inhibition at 10 μM (whole-cell patch-clamp recording) [1] - The compound showed high selectivity for TRESK over other two-pore domain potassium channels (K₂P): IC₅₀ > 10 μM for TREK1 (K₂P2.1), TRAAK (K₂P4.1), and TASK1 (K₂P3.1) [1] - No significant inhibition of voltage-gated potassium channels (KV1.1, KV2.1) or calcium-activated potassium channels (BKCa) was observed at concentrations up to 10 μM [1] - A2793 exhibited no obvious cytotoxicity to HEK293 cells at concentrations up to 20 μM (MTT assay), with cell viability >90% compared to vehicle control [1] |
| Enzyme Assay |
TRESK channel inhibition assay (whole-cell patch-clamp): HEK293 cells were transfected with human TRESK cDNA and cultured for 24–48 hours. Cells were placed in a recording chamber, and whole-cell patch-clamp configuration was established with a holding potential of -60 mV. Serial dilutions of A2793 were applied via perfusion, and TRESK channel currents were recorded. Current amplitude changes were analyzed to calculate inhibition rate and IC₅₀ value [1]
- K₂P channel selectivity assay: HEK293 cells expressing TREK1, TRAAK, or TASK1 were prepared similarly. A2793 (10 μM) was applied, and channel currents were recorded to evaluate cross-reactivity with other K₂P subtypes [1] |
| Cell Assay |
TRESK-expressing HEK293 cell culture and transfection: HEK293 cells were seeded in 35 mm dishes and transfected with human TRESK expression plasmid using transfection reagent. Cells were cultured in medium at 37°C with 5% CO₂ for 24–48 hours to allow TRESK expression [1]
- Whole-cell patch-clamp recording for TRESK activity: Transfected cells were visualized under an inverted microscope. Patch pipettes were filled with intracellular solution, and seal resistance >1 GΩ was achieved. After breaking into whole-cell mode, cells were perfused with extracellular solution containing A2793 at different concentrations. Currents were amplified, digitized, and analyzed with recording software [1] - Cytotoxicity assay: HEK293 cells were seeded in 96-well plates (1×10⁴ cells/well) and treated with A2793 (0.1–20 μM) for 72 hours. MTT reagent was added, and absorbance at 570 nm was measured to calculate cell viability [1] |
| References | |
| Additional Infomation |
A2793 is a chemically modified derivative of cloxyquin, designed as a selective TRESK (K₂P18.1) potassium channel inhibitor [1]
- Its mechanism of action involves directly blocking the pore domain of TRESK channel, suppressing background potassium conductance without affecting channel gating kinetics [1] - The compound is a valuable tool compound for studying TRESK channel physiology and pathophysiology, with potential applications in research on pain, migraine, and neurological disorders [1] - Compared to the parent compound cloxyquin (a TRESK activator), A2793 exerts opposite regulatory effects on TRESK channel activity, providing a complementary tool for K₂P channel research [1] |
| Molecular Formula |
C13H12CLNO3
|
|---|---|
| Molecular Weight |
265.692282676697
|
| Exact Mass |
265.051
|
| Elemental Analysis |
C, 58.77; H, 4.55; Cl, 13.34; N, 5.27; O, 18.06
|
| CAS # |
88349-90-0
|
| PubChem CID |
21933492
|
| Appearance |
White to off-white solid powder
|
| Density |
1.291±0.06 g/cm3
|
| Boiling Point |
393.4±27.0 °C
|
| LogP |
2.83
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
18
|
| Complexity |
287
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(COC1C2C(=CC=CN=2)C(Cl)=CC=1)OCC
|
| InChi Key |
JEMXUSHXYOXNFL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H12ClNO3/c1-2-17-12(16)8-18-11-6-5-10(14)9-4-3-7-15-13(9)11/h3-7H,2,8H2,1H3
|
| Chemical Name |
ethyl 2-(5-chloroquinolin-8-yl)oxyacetate
|
| Synonyms |
A2793; A-2793; A2793;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Animal Admin |
Chemical Formula | C₁₃H₁₂ClNO₃Morlecular Weight
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~376.38 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7638 mL | 18.8189 mL | 37.6378 mL | |
| 5 mM | 0.7528 mL | 3.7638 mL | 7.5276 mL | |
| 10 mM | 0.3764 mL | 1.8819 mL | 3.7638 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
