AMPAR/Nav1.2-IN-1
AMPAR/Nav1.2-IN-1 is a blood-brain barrier-penetrant AMPAR inhibitor and Nav1.2 blocker with IC50 values of 12.7 and 7.01 μM, respectively. AMPAR/Nav1.2-IN-1 inhibits AMPA-mediated excitatory currents and neuronal Nav1.2 voltage-gated sodium channels. AMPAR/Nav1.2-IN-1 scavenges free radicals via HAT and SET, increases GSH and SOD while decreasing MDA, and restores GABA-glutamate homeostasis by attenuating glutamate elevation and increasing GABA. AMPAR/Nav1.2-IN-1 can be used for epilepsy research.
For research use only. We do not sell to patients.
- Formula: C16H12N2O2S
- Molecular Weight:296.34
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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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Biological Activity
Description
IC50 & Target
[1]|
AMPAR 12.7 μM (IC50) |
Nav1.2 7.01 μM (IC50) |
In Vitro
AMPAR/Nav1.2-IN-1 inhibits AMPAR with an IC50 of 12.7 μM and has lower potency against NMDAR[1].
AMPAR/Nav1.2-IN-1 exhibits high blood-brain barrier permeability in the PAMPA-BBB assay, with a Pe of 18.70 × 10-6 cm/s[1].
AMPAR/Nav1.2-IN-1 shows minimal inhibition of CYP3A4, CYP2D6, and CYP2C9 (inhibition rates of 2.12%, 3.11%, and 4.07%, respectively)[1].
AMPAR/Nav1.2-IN-1 (200 μM) maintains >75% viability in PC12 and HEK293T cells[1].
AMPAR/Nav1.2-IN-1 inhibits cardiac NaV1.5 current by less than 10%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Tmax | Cmax | Vz/F | AUC0-∞ | MRT | Plasma Concentration |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 50 mg/kg | i.p. | 15 min | 72 μg/mL | 1.82 L/kg | 13347.9 mg/min/L | 218.3 min | / |
| Mice[1] | 50 mg/kg | i.p. | 30 min | / | / | / | 225.7 min | 41 μg/g |
| Mice[1] | 50 mg/kg | p.o. | 30 min | 40 ng/mL | 0.0092 L/min/kg | 10864 mg/min/L | 235.6 min | / |
| Mice[1] | 50 mg/kg | p.o. | 60 min | 24 μg/g | / | / | 248 min | / |
Chemical Information
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Molecular Weight 296.34
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Formula C16H12N2O2S
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SMILES
S=C(N1)N(C2=CC=C(OCO3)C3=C2)C=C1C4=CC=CC=C4
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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)
AMPAR/Nav1.2-IN-1 Related Classifications
HY-189650 Related Classifications
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