Kv7.2/Kv7.3 activator-2

Cat. No.: HY-172887: Data Sheet Handling Instructions
FAQs
Technical Support

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.

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

Kv7.2/Kv7.3 activator-2 Chemical Structure

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

KCNQ2/Q3

0.25 μM (EC₅₀)

In Vitro

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.

Parmacokinetics

Species	Dose	Route	Indicator	value
Mice	30 mg/kg	i.v.	AUC_0-∞	7922.2 ng·h/mL
Mice	30 mg/kg	p.o.	AUC_0-∞	3879.5 ng·h/mL
Mice	30 mg/kg	i.v.	AUC_0-t	7905.7 ng·h/mL
Mice	30 mg/kg	p.o.	AUC_0-t	3854.7 ng·h/mL
Mice	30 mg/kg	i.v.	C_max	19300 ng/mL
Mice	30 mg/kg	p.o.	C_max	4840 ng/mL
Mice	30 mg/kg	i.v.	CL	63.11 mL/min/kg
Mice	30 mg/kg	p.o.	CL	123.9 mL/min/kg
Mice	30 mg/kg	i.v.	MRT_0-∞	0.4 hr
Mice	30 mg/kg	p.o.	MRT_0-∞	1.2 hr
Mice	30 mg/kg	i.v.	T_1/2	1.97 hr
Mice	30 mg/kg	p.o.	T_1/2	1.00 hr
Mice	30 mg/kg	i.v.	T_max	0.083 hr
Mice	30 mg/kg	p.o.	T_max	0.100 hr
Mice	30 mg/kg	i.v.	B/P	0.23 (4h) %
Mice	30 mg/kg	p.o.	B/P	0.52 (4h) %
Mice	30 mg/kg	i.v.	B/P	0.56 (2h) %
Mice	30 mg/kg	p.o.	B/P	0.58 (2h) %
Mice	30 mg/kg	i.v.	V_z	10.74 L/kg
Mice	30 mg/kg	p.o.	F	49 %
Mice	30 mg/kg	p.o.	V_z	10.96 L/kg

In Vivo

Kv7.2/Kv7.3 activator-2 (Compound 2c) (1-100 mg/kg, i.p.) confers dose-dependent protection against maximal electroshock (MES)-induced acute mice seizure models with an ED₅₀ of 4.02 mg/kg, and protects 100% at 100 mg/kg dose^[1].
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.

Animal Model:	MES-induced acute seizure KM mice (6 weeks) model
Dosage:	1, 3, 10, 30, 100 mg/kg
Administration:	i.p., 30 min before electrically stimulation, and then mice were electrically stimulated and observed their seizure behavior.
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.

Animal Model:	sc-PTZ (100 mg/kg, i.p.)- induced acute seizure KM mice (6 weeks) model
Dosage:	1, 3, 10, 30, 50, 100 mg/kg
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.
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.

Animal Model:	KM mice (6 weeks)
Dosage:	100, 132, 174, 229, 303, 400, 528, and 679 mg/kg
Administration:	p.o., and then recorded the health status and mortality of the mice for 14 days post-administration.
Result:	had a safe therapeutic window of acute toxicity for antiepileptic effects with an LD₅₀ of 340.35 mg/kg.

Molecular Weight

300.42

Formula

C₁₇H₂₀N₂OS

SMILES

CC1=CC2=C(C(C)=C1NC(C3CC4CCC3C4)=O)SC=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zhang D, et al. Design, synthesis, and structure-activity relationship of 5, 7-dimethylbenzo [d] thiazoles as novel Kv7.2/7.3 activators with antiepileptic effects [J]. European Journal of Medicinal Chemistry, 2025: 117660.