QX-314 Br

Alias: QX-314 Br QX-314Br QX314 Br QX 314 QX314.
Cat No.:V13541 Purity: ≥98%
QX-314 Br is a novel intracellular blocker of NaVchannels1-4and a membrane impermeable quaternary analogue of lidocaine, a blocker of voltage-activated Na+ channels.
QX-314 Br Chemical Structure CAS No.: 24003-58-5
Product category: Sodium Channel
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
50mg
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Other Forms of QX-314 Br:

  • QX-314 chloride
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

QX-314 Br is a novel intracellular blocker of NaV channels1-4 and a membrane impermeable quaternary analogue of lidocaine, a blocker of voltage-activated Na+ channels. QX 314 bromide also inhibits calcium currents in hippocampal CA1 pyramidal neurons.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Transient receptor potential vanilloid subtype 1 (TRPV1) channels are subjected to biphasic effects by QX-314 bromide in vitro [1]. TRPV1 is immediately activated by QX-314 bromide (1–60 mM) in a concentration-dependent manner [1]. Cell death and blackening of the oocyte membrane are caused by QX-314 bromide (≥ 30 mM) [1]. In hippocampal CA1 pyramidal neurons, QX-314 bromide suppresses intracellular calcium currents, resulting in low-threshold (T-type) Ca2+ currents that average less than 10% of the control amplitude [3]. Because QX-314 bromide contains intracellular Br-, it causes a shift in the current-voltage relationship (IV) toward a positive voltage [3].
ln Vivo
QX-314 bromide (1.6 mg/kg; ic) eliminates reactions to painful mechanical and thermal stimuli when combined with capsaicin without causing impairments to motor or tactile function [2].
Animal Protocol
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (250-290 g) [2]
Doses: 1.6 mg/kg
Route of Administration: intradermal injection
Experimental Results: Response to noxious mechanical and thermal stimuli was eliminated when co-treated with capsaicin , without motor or tactile deficits.
References
[1]. Rivera-Acevedo RE, et al. The quaternary lidocaine derivative, QX-314, exerts biphasic effects on transient receptor potential vanilloid subtype 1 channels in vitro. Anesthesiology. 2011 Jun;114(6):1425-34.
[2]. Binshtok AM, et al. Coapplication of lidocaine and the permanently charged sodium channel blocker QX-314 produces a long-lasting nociceptive blockade in rodents. Anesthesiology. 2009 Jul;111(1):127-37.
[3]. Talbot MJ, et al. Intracellular QX-314 inhibits calcium currents in hippocampal CA1 pyramidal neurons. J Neurophysiol. 1996 Sep;76(3):2120-4.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H27BRN2O
Molecular Weight
343.30238
CAS #
24003-58-5
Related CAS #
QX-314 chloride;5369-03-9
SMILES
CC[N+](CC)(CC(NC1=C(C)C=CC=C1C)=O)CC.[Br-]
InChi Key
DLHMKHREUTXMCH-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H26N2O.BrH/c1-6-18(7-2,8-3)12-15(19)17-16-13(4)10-9-11-14(16)5/h9-11H,6-8,12H2,1-5H31H
Chemical Name
N-(2,6-Dimethylphenylcarbamoylmethyl)triethylammonium bromide
Synonyms
QX-314 Br QX-314Br QX314 Br QX 314 QX314.
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
H2O : ~100 mg/mL (~291.29 mM)
DMSO : ~50 mg/mL (~145.65 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 50 mg/mL (145.65 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.9129 mL 14.5645 mL 29.1290 mL
5 mM 0.5826 mL 2.9129 mL 5.8258 mL
10 mM 0.2913 mL 1.4565 mL 2.9129 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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