1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Sodium Channel Calcium Channel
  3. Nav1.2-IN-2

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.

Nav1.2-IN-2

Nav1.2-IN-2 Chemical Structure

CAS No. : 7469-49-0

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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target[1]

Nav1.2

0.18 μM (IC50)

In Vitro

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.

Parmacokinetics
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 / /
Molecular Weight

322.40

Formula

C17H26N2O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(C)C(NC(OCCCC)=O)=C1)OCCCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1017 mL 15.5087 mL 31.0174 mL
5 mM 0.6203 mL 3.1017 mL 6.2035 mL
View the 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.

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Purity & Documentation
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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Nav1.2-IN-2
Cat. No.:
HY-178963
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