| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Persistent Sodium Current (INaP) / Sodium Channels (Nav1.5, SCN8A)
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| ln Vitro |
Compared to the targeted antiepileptic medications carbamazepine and lamotrigine, relutrigine (0.001–10,000 µM) has a greater inhibitory action on hNaV1.6 sustained sodium channels. A consistent INa preference is seen in relutrigine. Wild-type CA1 pyramidal neurons exhibit a considerable reduction in intrinsic excitability upon exposure to 0.3 µM relutrine [1].
Relutrigine potently and preferentially inhibits persistent INa induced by ATX-II (Nav1.5 activator) or the SCN8A mutation N1768D with IC50 values of 141 nM and 75 nM, respectively. It exhibits use-dependent block, reducing neuronal intrinsic excitability. Its high selectivity for persistent current over transient peak current is key to its anticonvulsant effects. |
| ln Vivo |
In male CD-1 mice, relutrigine (0.3–40 mg/kg; oral; single dose) decreases movement distance and protects against tonic hindlimb epilepsy caused by maximum electroshock (MES) in a dosage-dependent manner[1].
In vivo studies demonstrate that Relutrigine has potent anticonvulsant activity in animal models of epilepsy, likely through reduction of neuronal hyperexcitability driven by persistent sodium current. It is being developed as a clinical-stage anticonvulsant for epilepsy, with potential for treating rare epilepsies linked to SCN8A mutations. |
| Enzyme Assay |
Recombinant human sodium channel isoforms (e.g., Nav1.5) are expressed in HEK293 cells. Whole-cell patch-clamp recordings are performed to measure sodium currents. Persistent INa is induced pharmacologically with ATX-II (1-10 microM) or by introducing the SCN8A N1768D mutation. Cells are held at a depolarized potential (e.g., -60 mV). Test compound is applied at varying concentrations, and the inhibition of sustained current is measured. IC50 values are calculated from dose-response curves.
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| Cell Assay |
HEK293 cells expressing wild-type Nav1.5 channels or SCN8A-N1768D mutant channels are cultured in DMEM with 10% FBS. Whole-cell patch-clamp electrophysiology is performed. Persistent sodium current is isolated using long depolarizing pulses (e.g., 500 ms) from a holding potential of -120 mV to -10 mV. For ATX-II induction, cells are pre-incubated with ATX-II (1-10 microM). Relutrigine is applied at 0.1-1000 nM, and the percentage of persistent current block is measured.
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| Animal Protocol |
Animal/Disease Models: Male CD-1 mice (~35 g; MES)[1].
Doses: 0.3, 1, 3, 10, 20 and 40 mg/kg. Route of Administration: Oral gavage; single dose. Experimental Results: demonstrated full anticonvulsant efficacy without affecting locomotor activity. In vivo studies are typically conducted in rodent models of epilepsy, including those with Scn8a mutations. Relutrigine is formulated in a suitable vehicle (e.g., 10% DMSO, 40% PEG300, 5% Tween 80, 45% saline) and administered orally (p.o.) or intraperitoneally (i.p.) at doses ranging from 1-30 mg/kg. Seizure activity is measured by EEG or behavioral observation. Efficacy is assessed as reduction in seizure frequency or severity. Data specific to Relutrigine are available from the developer. |
| ADME/Pharmacokinetics |
Relutrigine is orally bioavailable and long-acting, with a pharmacokinetic profile supporting once- or twice-daily dosing in preclinical species. Detailed PK parameters (e.g., half-life, Cmax, AUC, clearance) have been reported in the literature and by the developer, Praxis Precision Medicines.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies have been conducted to support clinical development. Relutrigine is generally well tolerated with no significant genotoxicity, cardiotoxicity (hERG, in vivo QT), or target organ toxicity at therapeutic doses. The no-observed-adverse-effect level (NOAEL) has been determined in 28-day and 90-day toxicology studies in rodent and non-rodent species.
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| References | |
| Additional Infomation |
Prax-562 is a small molecule drug. Its International Nonproprietary Name (INN) stem "-trigine" indicates that rilutrazine is a sodium channel blocker and signal transduction modulator. Rilutrazine is currently being investigated in the clinical trial NCT07010471 (a clinical trial evaluating the efficacy, safety, tolerability, and pharmacokinetics of rilutrazine in subjects with diabetic energy depletion disorder (DEE). The monoisotopic molecular weight of rilutrazine is 407.08 Da.
Relutrigine (PRAX-562) is a clinical-stage drug candidate developed by Praxis Precision Medicines for the treatment of epilepsy, including rare genetic epilepsies such as those associated with SCN8A mutations. It is designed to selectively target persistent sodium current (INaP) while sparing peak transient currents, potentially offering an improved side effect profile over traditional sodium channel blockers. As of 2026, it is not yet approved for clinical use; development status may have changed. References: Johnson JP Jr, et al. Mol Pharmacol. 2022;101(1):36-47. |
| Molecular Formula |
C15H11F6N5O2
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|---|---|
| Molecular Weight |
407.270563364029
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| Exact Mass |
407.081
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| CAS # |
2392951-29-8
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| PubChem CID |
147075611
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| Appearance |
White to light yellow solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
528
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C12=NN=C(C(OCC)(F)F)N1C=C(C1=CC(F)=C(OCC(F)(F)F)N=C1)N=C2
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| InChi Key |
BFXBSYMVTNEFRF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11F6N5O2/c1-2-28-15(20,21)13-25-24-11-5-22-10(6-26(11)13)8-3-9(16)12(23-4-8)27-7-14(17,18)19/h3-6H,2,7H2,1H3
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| Chemical Name |
3-[ethoxy(difluoro)methyl]-6-[5-fluoro-6-(2,2,2-trifluoroethoxy)pyridin-3-yl]-[1,2,4]triazolo[4,3-a]pyrazine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2455 mL | 1.2277 mL | 2.4554 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT05818553
Conditions:SCN2A Encephalopathy|SCN8A EncephalopathyLink: https://clinicaltrials.gov/ct2/show/NCT07010471
Conditions:Developmental and Epileptic Encephalopathy 1Products are for research use only; We do not sell to patients
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