产品
编 号：F751983
分子式：C15H11F6N5O2
分子量：407.27
分子式：C15H11F6N5O2
分子量：407.27
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2392951-29-8
产品详情
生物活性：
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.
体内研究：
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。Animal Model:Male CD-1 mice (~35 g; MES).
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.
体外研究：
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。
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.
体内研究：
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。Animal Model:Male CD-1 mice (~35 g; MES).
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.
体外研究：
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。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备