Relutrigine  (Synonyms: PRAX-562)

Relutrigine (PRAX-562) is an orally active inhibitor of persistent sodium channel. Relutrigine potently and preferentially inhibits persistent I_Na 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].

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

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

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].

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

407.27

C₁₅H₁₁F₆N₅O₂

2392951-29-8

FC1=C(OCC(F)(F)F)N=CC(C2=CN3C(C(F)(OCC)F)=NN=C3C=N2)=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]