| Identification | Back Directory | [Name]
1,2,4-Triazolo[4,3-a]pyrazine, 3-(ethoxydifluoromethyl)-6-[5-fluoro-6-(2,2,2-trifluoroethoxy)-3-pyridinyl]- | [CAS]
2392951-29-8 | [Synonyms]
1,2,4-Triazolo[4,3-a]pyrazine, 3-(ethoxydifluoromethyl)-6-[5-fluoro-6-(2,2,2-trifluoroethoxy)-3-pyridinyl]- | [Molecular Formula]
C15H11F6N5O2 | [MOL File]
2392951-29-8.mol | [Molecular Weight]
407.27 |
| Hazard Information | Back Directory | [Description]
Relutrigine is a sodium channel blocker. | [Uses]
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 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]. | 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. |
| [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. DOI:10.1111/epi.17149 |
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