1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. Lu AE98134

Lu AE98134 

Cat. No.: HY-133910 Purity: 98.37%
Handling Instructions

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.

For research use only. We do not sell to patients.

Lu AE98134 Chemical Structure

Lu AE98134 Chemical Structure

CAS No. : 849000-18-6

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5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
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25 mg USD 1050 In-stock
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50 mg USD 1650 In-stock
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100 mg USD 2600 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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].

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

425.50

Formula

C₂₁H₂₃N₅O₃S

CAS No.
SMILES

O=S(C1=CC=C(OC)C(C2=NN=C3N2N=C(C)C4=C3C=CC=C4)=C1)(NCCCC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (587.54 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3502 mL 11.7509 mL 23.5018 mL
5 mM 0.4700 mL 2.3502 mL 4.7004 mL
10 mM 0.2350 mL 1.1751 mL 2.3502 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.89 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.89 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Lu AE98134Lu AE 98134Lu AE-98134Sodium ChannelNa channelsNa+ channelsSchizophreniaInterneuronParvalbuminInhibitorinhibitorinhibit

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Product Name:
Lu AE98134
Cat. No.:
HY-133910
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