2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. Relutrigine

Relutrigine  (Synonyms: PRAX-562)

Cat. No.: HY-148792 Purity: 99.13%
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Relutrigine (PRAX-562) is an orally active inhibitor of persistent sodium channel. Relutrigine potently and preferentially inhibits persistent INa induced by ATX-II (Nav 1.5 activator) or the SCN8A mutation N1768D with IC50 values of 141 nM and 75 nM, respectively. Relutrigine exhibits potent use-dependent block and reduces neuronal intrinsic excitability. Relutrigine has effective anticonvulsant activity.

For research use only. We do not sell to patients.

Relutrigine Chemical Structure

Relutrigine Chemical Structure

CAS No. : 2392951-29-8

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1 mg USD 350 In-stock
5 mg USD 875 In-stock
10 mg USD 1400 In-stock
50 mg USD 3850 In-stock
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Based on 1 publication(s) in Google Scholar

Relutrigine Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Relutrigine (PRAX-562) is an orally active inhibitor of persistent sodium channel. Relutrigine potently and preferentially inhibits persistent INa induced by ATX-II (Nav 1.5 activator) or the SCN8A mutation N1768D with IC50 values of 141 nM and 75 nM, respectively. Relutrigine exhibits potent use-dependent block and reduces neuronal intrinsic excitability. Relutrigine has effective anticonvulsant activity[1].

In Vitro

Relutrigine (0.001-10000 µM) has a stronger inhibitory effect on hNaV1.6 sustained sodium channel (INa) when compared with targeted antiepileptic drugs Carbamazepine (HY-B0246) and Lamotrigine (HY-B0495). Relutrigine shows preference for persistent INa. Relutrigine (0.3 µM) significantly reduces the intrinsic excitability of wild-type CA1 pyramidal neurons[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Relutrigine Related Antibodies
In Vivo

Relutrigine (0.3-40 mg/kg; po; single dose) exhibits protection in maximal electroshock seizure (MES) induced tonic hindlimb seizures, and reduces movement distance with dose-dependent manner in male CD-1 mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CD-1 mice (~35 g; MES)[1].
Dosage: 0.3, 1, 3, 10, 20 and 40 mg/kg.
Administration: Oral gavage; single dose.
Result: Showed full anticonvulsant efficacy without affecting locomotor activity.
Clinical Trial
Molecular Weight

407.27

Formula

C15H11F6N5O2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

FC1=C(OCC(F)(F)F)N=CC(C2=CN3C(C(F)(OCC)F)=NN=C3C=N2)=C1
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 : 100 mg/mL (245.54 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 2.4554 mL 12.2769 mL 24.5537 mL
5 mM 0.4911 mL 2.4554 mL 4.9107 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (6.14 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (6.14 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 2.4554 mL 12.2769 mL 24.5537 mL 61.3843 mL
5 mM 0.4911 mL 2.4554 mL 4.9107 mL 12.2769 mL
10 mM 0.2455 mL 1.2277 mL 2.4554 mL 6.1384 mL
15 mM 0.1637 mL 0.8185 mL 1.6369 mL 4.0923 mL
20 mM 0.1228 mL 0.6138 mL 1.2277 mL 3.0692 mL
25 mM 0.0982 mL 0.4911 mL 0.9821 mL 2.4554 mL
30 mM 0.0818 mL 0.4092 mL 0.8185 mL 2.0461 mL
40 mM 0.0614 mL 0.3069 mL 0.6138 mL 1.5346 mL
50 mM 0.0491 mL 0.2455 mL 0.4911 mL 1.2277 mL
60 mM 0.0409 mL 0.2046 mL 0.4092 mL 1.0231 mL
80 mM 0.0307 mL 0.1535 mL 0.3069 mL 0.7673 mL
100 mM 0.0246 mL 0.1228 mL 0.2455 mL 0.6138 mL
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Relutrigine Related Classifications

Help & FAQs
  • 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.

Keywords:

Relutrigine2392951-29-8PRAX-562PRAX562PRAX 562Sodium ChannelNa channelsNa+ channelsMiceINaAnticonvulsantInhibitorinhibitorinhibit

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