Kv7.2/Kv7.3 activator-2
Kv7.2/Kv7.3 activator-2 is a BBB-penetrable Kv7.2/7.3 activator (EC50: 0.25 μM). Kv7.2/Kv7.3 activator-2 has good photostability. Kv7.2/Kv7.3 activator-2 has potently antiepileptic effects in maximal electroshock (MES) and sc-pentylenetetrazol (sc-PTZ)-induced acute mice seizure models.
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- Formule: C17H20N2OS
- Masse moléculaire:300.42
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Stockage:
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]
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Activité biologique
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Chemical Information
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Activité biologique
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KCNQ2/Q3 0.25 μM (EC50) |
Kv7.2/Kv7.3 activator-2 (Compound 2c) (10 μM) shows a 20% higher activation efficacy compared to Retigabine (RTG) [1].
Kv7.2/Kv7.3 activator-2 (10 μM) has not obviously influence on cardiac Kv7.1 channels compared to the positive Kv7.1 activator ML277 (HY-12343)[1].
Kv7.2/Kv7.3 activator-2 (10 μM) binds to the PD site of Kv7.2, with key residues (W236, F305, and L299) playing crucial roles in Kv7.2 channel’s activation[1].
Kv7.2/Kv7.3 activator-2 has a photostability advantage over RTG under irradiation at wavelengths of 254 nm and 365 nm at predetermined intervals (0-12 h)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC | Plasma Concentration | Clearance (CL) | MRT | T1/2 | Tmax | Brain-to-Plasma Ratio | Vz | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice | 30 mg/kg | i.v. | 7922.2 ng·h/mL | 19300 ng/mL | 63.11 mL/min/kg | 0.4 h | 1.97 h | 0.083 h | 0.23 (4h) % | 10.74 L/kg | / |
| Mice | 30 mg/kg | p.o. | 3879.5 ng·h/mL | 4840 ng/mL | 123.9 mL/min/kg | 1.2 h | 1.00 h | 0.100 h | 0.52 (4h) % | 10.96 L/kg | 49 % |
Kv7.2/Kv7.3 activator-2 (1-100 mg/kg, i.p.) reduces sc-pentylenetetrazol (sc-PTZ) -induced maximal behavioral seizure scores in a dose-dependent manner with an ED50 of 43.17 mg/kg, and the survival rate of mice increases at 10 mg/kg dose[1].
Kv7.2/Kv7.3 activator-2 (10-50 mg/kg, i.p.) dose-dependently effects mouse locomotor activity, and mice displayed motor function deficits at 50 mg/kg dose[1].
Kv7.2/Kv7.3 activator-2 (100-679 mg/kg, p.o.) has a safe acute toxicity for antiepileptic effects in KM mice with a LD50 of 340.35 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MES-induced acute seizure KM mice (6 weeks) model
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Dosage:1, 3, 10, 30, 100 mg/kg
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Administration:i.p., 30 min before electrically stimulation, and then mice were electrically stimulated and observed their seizure behavior.
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Result:Dose-dependently protected against MES-induced acute mice seizure models with an ED50 of 4.02 mg/kg, and protects 100% at 100 mg/kg dose.
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Animal Model:sc-PTZ (100 mg/kg, i.p.)- induced acute seizure KM mice (6 weeks) model
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Dosage:1, 3, 10, 30, 50, 100 mg/kg
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Administration:i.p., 30 min before sc-PTZ injection, and then recorded. maximum seizure score and measured the latency to generalized tonic-clonic seizures within 30 min.
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Result:Dose-dependently reduced sc-PTZ -induced maximal behavioral seizure scores with an ED50 of 43.17 mg/kg, and the survival rate of mice increases at 10 mg/kg dose.
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Animal Model:KM mice (6 weeks)
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Dosage:100, 132, 174, 229, 303, 400, 528, and 679 mg/kg
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Administration:p.o., and then recorded the health status and mortality of the mice for 14 days post-administration.
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Result:had a safe therapeutic window of acute toxicity for antiepileptic effects with an LD50 of 340.35 mg/kg.
Chemical Information
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Masse moléculaire 300.42
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Formule C17H20N2OS
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SMILES
CC1=CC2=C(C(C)=C1NC(C3CC4CCC3C4)=O)SC=N2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Kv7.2/Kv7.3 activator-2 Related Classifications
HY-172887 Related Classifications
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