Azetukalner
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.61%
- CAS No.: 1009344-33-5
- Formula: C23H29FN2O
- Molecular Weight:368.49
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Membrane Transporter/Ion Channel Compound Library
HY-L011
-
Clinical Compound Library
HY-L026
-
Drug Repurposing Compound Library
HY-L035
-
Neuroprotective Compound Library
HY-L070
-
Potassium Channel Compound Library
HY-L119
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Activators Library
HY-L159
-
Ion Channel Compound Library
HY-L166
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) Azetukalner
More
Biological Activity
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1009344-33-5
-
Appearance Solid
-
Molecular Weight 368.49
-
Formula C23H29FN2O
-
Color White to off-white
-
SMILES
O=C(CC(C)(C)C)NC1=C(C)C=C(N2CC3=CC=C(C=C3CC2)F)C=C1C
-
Synonyms
XEN1101
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
-
Journal Impact Factor
-
Most Recent
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Purity & Documentation
-
Data Sheet (272 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. Bialer M, et al. Progress report on new antiepileptic drugs: A summary of the Fifteenth Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XV). I. Drugs in preclinical and early clinical development. Epilepsia. 2020 Nov;61(11):2340-2364. [Content Brief]
[2]. Bialer M, et al. Progress report on new antiepileptic drugs: A summary of the Fourteenth Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XIV). I. Drugs in preclinical and early clinical development. Epilepsia. 2018 Oct;59(10):1811-1841. [Content Brief]
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 |
Azetukalner Related Classifications
HY-139791 Related Classifications
Powered by Bioz