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Lu AE98134

产品编号 T36813 CAS 849000-18-6

Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Nav1.1 channels positive modulator. Lu AE98134 also increases the activity of Nav1.2 and Nav1.5 channels but not of Nav1.4, Nav1.6 and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1].

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Lu AE98134, CAS 849000-18-6

规格	价格/CNY	货期
2 mg	待询	5日内发货
5 mg	￥ 10,980	5日内发货
25 mg	￥ 18,650	6-8周
50 mg	￥ 21,500	6-8周
100 mg	￥ 28,600	6-8周
1 mL * 10 mM (in DMSO)	待询	5日内发货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Nav1.1 channels positive modulator. Lu AE98134 also increases the activity of Nav1.2 and Nav1.5 channels but not of Nav1.4, Nav1.6 and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1].
体外活性	Lu AE98134 (30 μM) promotes the current mediated by Navv1.1 channel, and it activates Nav1.5 and to a lesser extent Nav1.2 but has no effect on Nav1.4, Nav1.6 and Nav1.7 currents in HEK cells expressing Nav1.1, Nav1.2, Nav1.6, Nav1.5, and Nav1.7 by step-wise depolarizing voltages using the whole-cell patchclamp configuration[1]. Lu AE98134 (30 μM) increases the excitability of FSINs by decreasing the threshold for action potentials.Intracellular depolarizing current pulses evokes repetitive firing of action potentials at frequencies, additionally, Lu AE98134 increases the excitability since each current pulse generated a higher number of spikes (163 spikes in control; and 230 spikes in Lu AE98134)[1].
体内活性	The fast spiking inhibitory interneurons (FSINs) from Dlx5/6+/- animals exhibit abnormal excitability because of a more depolarized spike threshold and broader action potentials.Lu AE98134 (30 μM) increases the excitability of FSINs neurons from normal and Dlx5/6+/- animals by modulating several parameters characteristic for NaV1.1 channels. The selective activation of FSINs by Lu AE98134 restores cognitive flexibility in adult Dlx5/6+/- mice[1].

分子量	425.5
分子式	C21H23N5O3S
CAS No.	849000-18-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 250 mg/mL (587.54 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3502 mL	11.7509 mL	23.5018 mL	58.7544 mL
	5 mM	0.47 mL	2.3502 mL	4.7004 mL	11.7509 mL
	10 mM	0.235 mL	1.1751 mL	2.3502 mL	5.8754 mL
	20 mM	0.1175 mL	0.5875 mL	1.1751 mL	2.9377 mL
	50 mM	0.047 mL	0.235 mL	0.47 mL	1.1751 mL
	100 mM	0.0235 mL	0.1175 mL	0.235 mL	0.5875 mL

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参考文献

1. Nadia Lyb?l von Schoubye, et al. The sodium channel activator Lu AE98134 normalizes the altered firing properties of fast spiking interneurons in Dlx5/6 +/- mice. Neurosci Lett. 2018 Jan 1;662:29-35.

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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