Relutrigine_product_DataBase

Bioactivity	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].
Invitro	Relutrigine (0.001-10000 µM) 对 hNaV1.6 持续钠通道具有更强的抑制作用，当与靶向抗癫痫药物卡马西平 (HY-B0246) 和拉莫三嗪 (HY-B0495) 相比。Relutrigine 显示出持久 INa 偏好。Relutrine (0.3 µM) 显著降低野生型 CA1 锥体神经元的内在兴奋性[1]。
In Vivo	Relutrigine (0.3-40 mg/kg；口服；单剂量) 在雄性 CD-1 小鼠内，以剂量依赖性方式保护最大电休克发作 (MES) 诱导的强直性后肢癫痫，并减少移动距离[1]。 Animal Model:
Name	Relutrigine
CAS	2392951-29-8
Formula	C15H11F6N5O2
Molar Mass	407.27
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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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