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

For research use only. We do not sell to patients.

E0714

E0714 Chemical Structure

CAS No. : 1359358-36-3

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E0714 Related Antibodies

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Description

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[1].

IC50 & Target[1]

KV7.2

1.90 μM (EC50)

Kv7.2/7.3

0.021 μM (EC50)

In Vitro

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.

E0714 Related Antibodies
Parmacokinetics
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 %
In Vivo

E0714 (1.25-20 mg/kg; i.p.) dose-dependently reduces the seizure severity induced by pentylenetetrazol (PTZ) in KM mice[1].
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.
Molecular Weight

347.37

Formula

C20H17N3O3
CAS No.
SMILES

CNC(C1=CC=CN(C1=O)C2=CC=C(C=C2)NC(C3=CC=CC=C3)=O)=O
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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E0714 Related Classifications

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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:

E07141359358-36-3E 0714E-0714Potassium ChannelKcsAVSD-PD cleftheteromeric Kv7.2/7.3 channelsneuronal resting membrane potentialKv7.2 potassium channelC57BL/6J miceblood-brain barrierKv7 family subtypehomomeric Kv7.2 channelsepilepsyKM miceInhibitorinhibitorinhibit

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