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。
生物活性 | Nav1.1 activator 1 (compound 4), a highly potentNav1.1activator withBBB penetration, increases decay time constant (tau) ofNav1.1currents at 0.03 μM along with significant selectivity againstNav1.2,Nav1.5, andNav1.6[1]. |
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体内研究 (In Vivo) | Nav1.1 activator 1 (compound 4) is a valuable Nav1.1 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[1].
Animal Model: | Mice[1]. | 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 Nav1.1 activator can restore Nav1.1 functions and modify the disease state in animal models. Could penetrate the blood-brain barrier (BBB) in humans.
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(567.59 mM;Need ultrasonic) 配制储备液 1 mM | 2.2704 mL | 11.3518 mL | 22.7035 mL | 5 mM | 0.4541 mL | 2.2704 mL | 4.5407 mL | 10 mM | 0.2270 mL | 1.1352 mL | 2.2704 mL |
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以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.72 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.08 mg/mL (4.72 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (4.72 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.72 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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