2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. Azetukalner

Azetukalner (XEN1101) is a selective and orally active Kv7.2/Kv7.3 potassium channel opener with an EC50 of 27 nM. Azetukalner is approximately 4-fold more selective for Kv7.2/7.3 over Kv7.3/7.5 (EC50 of 94 nM) and Kv7.4 (EC50 of 113 nM) channels. Azetukalner exhibits a selectivity >100-fold for Kv7 channels over other ion channels and receptors. Azetukalner can be used for the study of focal epilepsy.

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Azetukalner

Azetukalner Chemische Struktur

CAS. Nr. : 1009344-33-5

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10 mM * 1 mL in DMSO
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Azetukalner Related Antibodies

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Beschreibung

Azetukalner (XEN1101) is a selective and orally active Kv7.2/Kv7.3 potassium channel opener with an EC50 of 27 nM. Azetukalner is approximately 4-fold more selective for Kv7.2/7.3 over Kv7.3/7.5 (EC50 of 94 nM) and Kv7.4 (EC50 of 113 nM) channels. Azetukalner exhibits a selectivity >100-fold for Kv7 channels over other ion channels and receptors. Azetukalner can be used for the study of focal epilepsy[1][2].

In Vitro

In patch clamp studies conducted with HEK cells expressing KV7.2/7.3 channels, Azetukalner (EC50 of 42 nM) is found to be ~22 times more potent than Retigabine (EC50 of 920 nM) for causing an approximate −40-mV leftward shift in the half-maximal voltage of activation for the channel, while producing a similar increase in maximal conductance (ΔGmax = ~38% vs vehicle)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Azetukalner Related Antibodies
In Vivo

Azetukalner is effective in several models of electrically and chemically induced seizures in rodents. In comparison to retigabine in the electroshock (MES) test, using a 60-Hz bipolar stimulus with CF-1 mice. Under the conditions of this assay, Azetukalner reduces the fraction of mice seizing with a half-maximal effective concentration (EC50), based on plasma concentrations at time of testing, of 220 nM, which is 16-fold more potent than Retigabine (EC50 = 3500 nM)[1].
Studies in nonhuman primates showed a favorable pharmacokinetic profile of Azetukalner; for example, a single oral gavage dose of 1 mg/kg resulted in a Cmax of 54.2 ng/mL in male and 68.7 ng/mL in female monkeys, with an elimination half-life of 10.2 and 8.4 hours, respectively[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Klinische Studie
Molekulargewicht

368.49

Formel

C23H29FN2O
CAS. Nr.
Appearance

Solid

Color

Off-white to gray

SMILES

O=C(CC(C)(C)C)NC1=C(C)C=C(N2CC3=CC=C(C=C3CC2)F)C=C1C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 50 mg/mL (135.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7138 mL 13.5689 mL 27.1378 mL
5 mM 0.5428 mL 2.7138 mL 5.4276 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation

Purity: 99.61%

SDS (393 KB)

COA (244 KB) HNMR (263 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
Verweise

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7138 mL 13.5689 mL 27.1378 mL 67.8444 mL
5 mM 0.5428 mL 2.7138 mL 5.4276 mL 13.5689 mL
10 mM 0.2714 mL 1.3569 mL 2.7138 mL 6.7844 mL
15 mM 0.1809 mL 0.9046 mL 1.8092 mL 4.5230 mL
20 mM 0.1357 mL 0.6784 mL 1.3569 mL 3.3922 mL
25 mM 0.1086 mL 0.5428 mL 1.0855 mL 2.7138 mL
30 mM 0.0905 mL 0.4523 mL 0.9046 mL 2.2615 mL
40 mM 0.0678 mL 0.3392 mL 0.6784 mL 1.6961 mL
50 mM 0.0543 mL 0.2714 mL 0.5428 mL 1.3569 mL
60 mM 0.0452 mL 0.2261 mL 0.4523 mL 1.1307 mL
80 mM 0.0339 mL 0.1696 mL 0.3392 mL 0.8481 mL
100 mM 0.0271 mL 0.1357 mL 0.2714 mL 0.6784 mL
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Azetukalner Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Azetukalner1009344-33-5XEN1101XEN 1101XEN-1101Potassium ChannelKcsAKCNQ2/3activatorpotassium channelpainInhibitorinhibitorinhibit

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