Nav1.1 activator 1
| 中文名称 | Nav1.1 activator 1 |
|---|---|
| 中文同义词 | 化合物 T12179 |
| 英文名称 | Nav1.1 activator 1 |
| 英文同义词 | Nav1.1 activator 1;Nav1.1 activator 1,Nav-1.1 activator 1;3-Pyridinecarboxamide, 4-(2,5-difluorophenyl)-2-[(3S)-3-fluoro-1-pyrrolidinyl]-N-[6-(1-methylethyl)-3-pyridinyl]- |
| CAS号 | 2332897-85-3 |
| 分子式 | C24H23F3N4O |
| 分子量 | 440.46 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 2332897-85-3.mol |
| 结构式 |  |
Nav1.1 activator 1 性质
| 沸点 | 533.1±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.32±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 酸度系数(pKa) | 11.63±0.70(Predicted) |
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。
Na v 1.1.
Nav1.1 activator 1 (compound 4) is a valuable Na v 1.1 activator for further evaluation of pathophysiological functions of the Nav1.1 channel and has potential for therapeutic treatments of CNS diseases such as Dravet syndrome.
| Animal Model: | Mice. |
| Dosage: | 30 mg/kg ( Pharmacokinetic Analysis ). |
| Administration: | IP once (Exposure was measured at 1 h after administration). |
| Result: |
Intraperitoneal administration (30 mg/kg) of compound resulted in sufficient brain exposure (193 ng/g 1 h after administration), which corresponded to 13 nM of free brain concentration comparable to the in vitro potency of the compound.
Had a potential use as an in vivo tool to investigate whether this type of Na v 1.1 activator can restore Na v 1.1 functions and modify the disease state in animal models. Could penetrate the blood-brain barrier (BBB) in humans. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-126429 | Nav1.1 activator 1 | 1 mg | 1409元 | |
| 2024/04/30 | HY-126429 | Nav1.1 activator 1 Nav1.1 activator 1 | 2332897-85-3 | 5mg | 3100元 |