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標(biāo)簽:Lu AE98134
聯(lián)系人:高小姐
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化學(xué)性質(zhì):
規(guī)格 | 5 mg 10 mg 25 mg 50 mg 100 mg |
CAS | 849000-18-6 |
別名 | N/A |
化學(xué)名 | N/A |
分子式 | C21H23N5O3S |
分子量 | 425.5 |
溶解度 | DMSO: 250 mg/mL (587.54 mM) |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產(chǎn)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].
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].
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].
[1]. Nadia LybØl 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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原創(chuàng)作者:上海莼試生物技術(shù)有限公司
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賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業(yè)部
賬 號:2169 2341 6278