Nav1.1 activator 1

• 常用名: Nav1.1 activator 1
• 英文名: Nav1.1 activator 1
• CAS号: 2332897-85-3
• 分子量: 440.46
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₄H₂₃F₃N₄O
• 熔点: N/A
• 闪点: N/A

Nav1.1 activator 1用途

Nav1.1 activator 1 (compound 4) 是强有效的、能透过血脑屏障的、 Nav1.1 激动剂,0.03 μM 可增加衰减Nav1.1 电流的时间常数 τ。对 Nav1.2、Nav1.5、Nav1.6 有显著的选择性。

Nav1.1 activator 1名称

• 英文名: Nav1.1 activator 1

Nav1.1 activator 1生物活性

• 描述: Nav1.1 activator 1 (compound 4) 是强有效的、能透过血脑屏障的、 Nav1.1 激动剂,0.03 μM 可增加衰减Nav1.1 电流的时间常数 τ。对 Nav1.2、Nav1.5、Nav1.6 有显著的选择性。
• 相关类别:
  信号通路 >> 跨膜转运 >> 钠通道
  研究领域 >> 神经疾病
• 靶点实验:

  Nav1.1[1].

• 体内研究: Nav1.1激活剂1(化合物4)是一种有价值的Nav1.1激活剂,可用于进一步评价Nav1.1通道的病理生理功能,对中枢神经系统疾病如Dravet综合征具有潜在的治疗作用[1]。动物模型：小鼠[1]。剂量：30mg/kg(药代动力学分析)。给药：IP一次(给药后1h测量暴露量)。结果：腹腔给药(30mg/kg)可使大鼠足量脑暴露(给药后1h为193ng/g),相当于13nm的自由脑浓度,与化合物的体外药效相当。有可能作为一种体内工具来研究这种类型的Nav1.1激活剂能否在动物模型中恢复Nav1.1的功能和改变疾病状态。能穿透人的血脑屏障。
• 参考文献:

  [1]. Miyazaki T, et al. Discovery of novel 4-phenyl-2-(pyrrolidinyl)nicotinamide derivatives as potent Nav1.1 activators. Bioorg Med Chem Lett. 2019 Mar 15;29(6):815-820.

Nav1.1 activator 1物理化学性质

• 分子式: C₂₄H₂₃F₃N₄O
• 分子量: 440.46
• InChIKey: HRGJTEFGFUJXIF-INIZCTEOSA-N
• SMILES: CC(C)c1ccc(NC(=O)c2c(-c3cc(F)ccc3F)ccnc2N2CCC(F)C2)cn1

Nav1.1 activator 1靶点实验

查看更多实验

实验名称：Activation of human Nav1.1 expressed in T-Rex-CHO cells assessed as change in decay t... 来源：ChEMBL 靶标：Sodium channel protein type 1 subunit alpha External Id：CHEMBL4424231

实验名称：Activation of human Nav1.1 expressed in T-Rex-CHO cells assessed as change in decay t... 来源：ChEMBL 靶标：Sodium channel protein type 1 subunit alpha External Id：CHEMBL4424232

实验名称：Efflux ratio of permeability across pig LLC-PK1 cells expressing human MDR1 at 1 uM a... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4424233

实验名称：Drug uptake in mouse plasma at 30 mg/kg, ip measured at 1 hr by LC-MS/MS analysis 来源：ChEMBL 靶标：N/A External Id：CHEMBL4424234

实验名称：Drug uptake in mouse brain at 30 mg/kg, ip measured at 1 hr by LC-MS/MS analysis 来源：ChEMBL 靶标：N/A External Id：CHEMBL4424235

实验名称：Ratio of drug level in brain to plasma in mouse at 30 mg/kg, ip measured at 1 hr by L... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4424236

实验名称：Fraction unbound in mouse brain at 30 mg/kg, ip measured at 1 hr by LC-MS/MS analysis 来源：ChEMBL 靶标：N/A External Id：CHEMBL4424237

实验名称：Activation of human Nav1.1 expressed in T-Rex-CHO cells assessed as change in decay t... 来源：ChEMBL 靶标：Sodium channel protein type 1 subunit alpha External Id：CHEMBL4424223

实验名称：Activation of human Nav1.1 expressed in T-Rex-CHO cells assessed as change in top pea... 来源：ChEMBL 靶标：Sodium channel protein type 1 subunit alpha External Id：CHEMBL4424229

实验名称：Activation of human Nav1.1 expressed in T-Rex-CHO cells assessed as change in decay t... 来源：ChEMBL 靶标：Sodium channel protein type 1 subunit alpha External Id：CHEMBL4424230

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