Nav1.2-IN-3
Nav1.2-IN-3 is a blood-brain barrier-penetrant and potent voltage-gated sodium channel NaV1.2 inhibitor with an IC50 of 16.93 μM. Nav1.2-IN-3 preferentially blocks the inactivated state of the channel, inhibits neuronal hyperexcitability, and alleviates oxidative stress. Nav1.2-IN-3 can be used for research on epilepsy.
For research use only. We do not sell to patients.
- Formula: C18H14ClNO
- Molecular Weight:295.76
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
hNav1.2 16.93 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
>500 μM
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Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for a specified period by MTT assay.
Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for a specified period by MTT assay.
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42603541 |
| SH-SY5Y | IC50 |
>500 μM
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Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for a specified period by MTT assay.
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for a specified period by MTT assay.
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42603541 |
In Vitro
12a potently inhibits NaV1.2 channels with an IC50 of 16.93 μM and preferentially blocks the inactivated state[1].
12a exhibits low cytotoxicity in HEK293T and SH-SY5Y cell lines with an IC50 > 500 μM[1].
12a produces only minimal blockade of cardiac NaV1.5 channels at 50 μM, with 11.0% inhibition and an IC50 > 50 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
Nav1.2-IN-3 (30 mg/kg; i.p.; single administration; given 30 min before modeling) shows 60% protection against mortality and significantly prolongs clonic latency in the PTZ-induced acute seizure mouse model[1].
Nav1.2-IN-3 (i.p.; daily administration; for 15 consecutive days) significantly delays seizure progression, restores neurotransmitter balance, and alleviates oxidative stress in a chronic PTZ-kindled mouse model[1].
Nav1.2-IN-3 (30 mg/kg; i.p.; for 7 consecutive days) exhibits excellent hepatic safety in a mouse model for hepatotoxicity assessment, without causing liver injury[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss albino mice (modeled by electrical stimulation of 50 mA, 0.2 s, 60 Hz via ear clips) [1]
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Dosage:30 mg/kg
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Administration:i.p.; single dose; administered 30 minutes before electroshock
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Result:
Protected 100% of mice from electroshock-induced tonic hind limb extension (THLE) and provided 100% protection against mortality at a dose of 30 mg/kg.
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Animal Model:Swiss albino mice (modeled by i.p. injection of 85 mg/kg PTZ)[1]
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Dosage:30 mg/kg
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Administration:i.p.; single dose; administered 30 minutes before electroshock
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Result:Demonstrated activity providing 60% protection against death and significantly prolonging the latency of clonic seizures.
Chemical Information
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Molecular Weight 295.76
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Formula C18H14ClNO
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SMILES
O=C(CNC1=CC=CC=C1Cl)C2=CC3=C(C=C2)C=CC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Nav1.2-IN-3 Related Classifications
HY-189469 Related Classifications
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