2332897-85-3
中文名稱
Nav1.1 activator 1
英文名稱
Nav1.1 activator 1
CAS
2332897-85-3
分子式
C24H23F3N4O
分子量
440.46
MOL 文件
2332897-85-3.mol
2332897-85-3 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點(diǎn)533.1±50.0 °C(Predicted)
密度1.32±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
酸度系數(shù)(pKa)11.63±0.70(Predicted)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
Nav1.1 activator 1 (compound 4) 是強(qiáng)有效的、能透過血腦屏障的、 Nav1.1 激動(dòng)劑，0.03 μM 可增加衰減Nav1.1 電流的時(shí)間常數(shù) τ。對(duì) Nav1.2、Nav1.5、Nav1.6 有顯著的選擇性。靶點(diǎn)
Na v 1.1.
體內(nèi)研究
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. |