E0714
E0714 is a blood-brain barrier-permeable, selective Kv7.2 potassium channel activator, with EC50 values of 1.90 μM and 0.021 μM for homotetrameric Kv7.2 channels and heterotetrameric Kv7.2/7.3 channels, respectively. E0714 exhibits anticonvulsant activity. E0714 can be used in research related to epilepsy.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 1359358-36-3
- Fòrmula: C20H17N3O3
- Peso molecular:347.37
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
|
KV7.2 1.90 μM (EC50) |
Kv7.2/7.3 0.021 μM (EC50) |
E0714 potently and selectively activates wild-type Kv7.2 homomeric channels and Kv7.2/Kv7.3 heteromeric channels, with an EC50 of 1.90 ± 0.70 μM for activating Kv7.2 currents[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | Vz-F_obs | ClF_obs | MRT0-t | MRT0-∞ | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 5.17 h | 0.167 h | 1059.40 μg/L | 9830.43 μg/L·h | 9907.77 μg/L·h | 0.79 L/kg | 0.10 L/h/kg | 7.62 h | 7.92 h | / |
| Rat[1] | 5 mg/kg | p.o. | 6.27 h | 2.00 h | 3288.34 μg/L | 36858.68 μg/L·h | 37327.95 μg/L·h | 0.95 L/kg | 0.14 L/h/kg | 10.01 h | 11.29 h | 75.35 % |
E0714 (1.25-20 mg/kg; i.p.) dose-dependently protects KM mice against MES-induced seizures, with an ED50 of 2.45 mg/kg, and achieves 100% protective efficacy at the dose of 20 mg/kg[1].
E0714 (1.25-20 mg/kg; i.p.; once daily; for 3 consecutive days) dose-dependently reduces the incidence and duration of seizures induced by 6 Hz stimulation in C57BL/6J mice, with an ED50 of 3.56 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:KM (male, SPF grade, 18-20 g, pentylenetetrazol-induced seizure model)[1]
-
Dosage:1.25-20 mg/kg
-
Administration:i.p.
-
Result:Prolonged latency to stage 3 or higher seizures and reduced total maximum seizure grade score within 30 minutes at all doses compared to vehicle.
Extended seizure onset latency at 1.25 mg/kg but did not significantly reduce stage 5 seizure duration.
Showed superior antiseizure efficacy to retigabine at equivalent 10 mg/kg doses.
Achieved a median effective dose (ED50) of 4.29 mg/kg (95% confidence interval: 1.86-6.78 mg/kg) for reducing total seizure score.
Chemical Information
-
No. CAS 1359358-36-3
-
Peso molecular 347.37
-
Fòrmula C20H17N3O3
-
SMILES
CNC(C1=CC=CN(C1=O)C2=CC=C(C=C2)NC(C3=CC=CC=C3)=O)=O
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
E0714 Related Classifications
HY-181874 Related Classifications
Powered by Bioz