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.
All iGluR Isoforms
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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. Further protocols information, click here.
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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.
Protocols
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)