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Relutrigine

カタログ番号GC71053

Relutrigine (prax-562)は、持続性ナトリウムチャネルの経口活性阻害剤である。

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Relutrigine 化学構造

Cas No.: 2392951-29-8

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$635.00
在庫あり
1 mg
$322.00
在庫あり
5 mg
$709.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents
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.

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