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Relutrigine

Catalog No.GC71053 Copy One-Click Copy Product Info

Relutrigine (PRAX-562) is an orally active inhibitor of persistent sodium channel.

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Relutrigine Chemical Structure

Cas No.: 2392951-29-8

Size Price Stock Qty
10mM (in 1mL DMSO)
$635.00
In stock
1 mg
$322.00
In stock
5 mg
$709.00
In stock

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Sample solution is provided at 25 µL, 10mM.



Description of Relutrigine

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.

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

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].

References:
[1]. Kahlig KM, et al. The novel persistent sodium current inhibitor PRAX-562 has potent anticonvulsant activity with improved protective index relative to standard of care sodium channel blockers. Epilepsia. 2022 Mar;63(3):697-708.

Chemical Properties of Relutrigine

Cas No. 2392951-29-8 SDF
Formula C15H11F6N5O2 M.Wt 407.27
Solubility 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) Storage -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Relutrigine

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.4554 mL 12.2769 mL 24.5537 mL
5 mM 491.1 μL 2.4554 mL 4.9107 mL
10 mM 245.5 μL 1.2277 mL 2.4554 mL
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In vivo Formulation Calculator (Clear solution) of Relutrigine

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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