Dual Nav/NMDAR-IN-1
Dual Nav/NMDAR-IN-1 (compound 11a) is a dual-target modulator of Nav and NMDAR. Dual Nav/NMDAR-IN-1 increases the thermal stability of Nav and NMDAR and slows their proteolytic degradation, indicating that it binds to both Nav and NMDAR simultaneously. Dual Nav/NMDAR-IN-1 exhibits anticonvulsant activity in a pentylenetetrazole-induced mouse model of seizures and can be used in epilepsy-related research.
For research use only. We do not sell to patients.
- Formula: C30H44N4O5
- Molecular Weight:540.69
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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
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Biological Activity
Description
IC50 & Target
[1]|
Nav |
NMDAR |
In Vitro
Dual Nav/NMDAR-IN-1 (compound 11a) (100 μM; 48 h) exhibits low cytotoxicity, with >70% cell viability across AC16, HEK-293 T, LX-2, and SH-SY5Y human cell lines when treated at 100 μM for 48 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AC16, HEK-293 T, LX-2, SH-SY5Y
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Concentration:100 μM
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Incubation Time:48 h
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Result:Maintained 86.64% viability in AC16 cells.
Maintained 86.25% viability in HEK-293 T cells.
Maintained 81.91% viability in LX-2 cells.
Maintained 76.56% viability in SH-SY5Y cells.
In Vivo
Dual Nav/NMDAR-IN-1 (50-200 mg/kg; i.p.; once daily; for 7 consecutive days) exhibits dose-dependent in vivo safety: no mice die at the dose of 50 mg/kg, while 4 out of 8 mice survive after 7 consecutive days of daily i.p. administration at 200 mg/kg, which is consistent with the mortality of all test compounds at high doses[1].
Dual Nav/NMDAR-IN-1 (50-200 mg/kg; i.p.; single administration) exhibits mild dose-dependent neurotoxicity at the dose of 200 mg/kg, while no neurotoxicity is observed at 50 mg/kg following a single intraperitoneal injection[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kunming (KM) strain (male, 3-4 weeks old, 20-22 g)[1]
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Dosage:50 mg/kg
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Administration:i.p.; 2 h before PTZ challenge
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Result:Prolonged first clonic seizure latency from 76.3 to 179.0 s and reduced the Racine score from 5.25 to 3.13.
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Animal Model:(male, 3-4 weeks old)[1]
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Dosage:200 mg/kg; 50 mg/kg
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Administration:i.p.; daily; 7 days
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Result:No mortality at 50 mg/kg; 4 of 8 mice survived through day 7 at 200 mg/kg.
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Animal Model:(male, 3-4 weeks old)[1]
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Dosage:200 mg/kg; 50 mg/kg
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Administration:i.p.; single dose
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Result:No neurotoxicity at 50 mg/kg; at 200 mg/kg, neurotoxicity occurred in 1/8 mice at 0.5 h and 3/8 mice at 4 h.
Chemical Information
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Molecular Weight 540.69
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Formula C30H44N4O5
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SMILES
O=C(NCCCC(NC12CC3(C)CC(C2)(C)CC(C3)C1)=O)C4=CC=C(CNC([C@H](NC(C)=O)COC)=O)C=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)
Dual Nav/NMDAR-IN-1 Related Classifications
HY-184718 Related Classifications
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