Nav1.2-IN-2
Based on 1 Customer Validation
Nav1.2-IN-2 is a Nav1.2 inhibitor with a human IC50 of 0.18 μM. Nav1.2-IN-2 preferentially binds to the inactivated state of Nav1.2, reduces window current, suppresses neuronal depolarization and action potential generation. Nav1.2-IN-2 suppresses Veratridine (HY-N6691)-induced Ca2+ influx. Nav1.2-IN-2 can be used for the research of epilepsy.
For research use only. We do not sell to patients.
- Purity: 99.82%
- CAS No.: 7469-49-0
- Formula: C17H26N2O4
- Molecular Weight:322.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Calcium Channel Isoforms
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Biological Activity
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Nav1.2 0.18 μM (IC50) |
Nav1.2-IN-2 (Compound 1) (0.1-10 μM; 15 min) potently suppresses spontaneous synchronized Ca2+ oscillation amplitude and frequency in primary cultured neocortical neurons with IC50 values of 0.38 μM and 0.88 μM, respectively[1].
Nav1.2-IN-2 (0.1-10 μM; 15 min) potently inhibits Veratridine-induced Ca2+ influx in primary cultured neocortical neurons with an IC50 of 1.89 μM[1].
Nav1.2-IN-2 exhibits state-dependent inhibition of Nav1.2 in transiently transfected HEK-293 cells, shifting steady-state inactivation hyperpolarization by 10.99 mV and inhibiting the inactivated state with an IC50 of 0.18 μM, while having no effect on steady-state activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-∞ | AUClast | CL | Cmax | MRT0-∞ | T1/2 | Tmax | Vd | F | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 30759 ng·h/mL | 29767 ng·h/mL | / | 1060 ng/mL | 19.4 h | 20.1 h | 8.00 h | / | 64.3 % | / |
| Mice[1] | 1 mg/kg | i.v. | 5063 ng·h/mL | 4776 ng·h/mL | 201 mL/h/kg | 849 ng/mL | 10.4 h | 8.47 h | 0.08 h | 2.37 L/kg | / | / |
| Rat[1] | 10 mg/kg | p.o. | 4684 ng·h/mL | 5618 ng·h/mL | / | 343 ng/mL | 11.4 h | 7.73 h | 4.67 h | / | / | 14.07 % |
| Rat[1] | 1 mg/kg | i.v. | 5005 ng·h/mL | 4676 ng·h/mL | 203 mL/h/kg | 1247 ng/mL | 9.50 h | 8.52 h | 0.08 h | 2.49 L/kg | / | / |
Chemical Information
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CAS No. 7469-49-0
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Appearance Solid
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Molecular Weight 322.40
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Formula C17H26N2O4
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Color White to off-white
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SMILES
O=C(NC1=CC=C(C)C(NC(OCCCC)=O)=C1)OCCCC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 4.17 mg/mL (12.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (267 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1017 mL | 15.5087 mL | 31.0174 mL | 77.5434 mL |
| 5 mM | 0.6203 mL | 3.1017 mL | 6.2035 mL | 15.5087 mL | |
| 10 mM | 0.3102 mL | 1.5509 mL | 3.1017 mL | 7.7543 mL |