QX-314 Br
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 532485

CAS#: 24003-58-5

Description: QX-314 Br is a membrane impermeable quaternary derivative of lidocaine, a blocker of voltage-activated Na+ channels. QX 314 bromide also inhibits calcium currents in hippocampal CA1 pyramidal neurons.


Chemical Structure

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QX-314 Br
CAS# 24003-58-5

Theoretical Analysis

MedKoo Cat#: 532485
Name: QX-314 Br
CAS#: 24003-58-5
Chemical Formula: C16H27BrN2O
Exact Mass: 0.00
Molecular Weight: 343.310
Elemental Analysis: C, 55.98; H, 7.93; Br, 23.27; N, 8.16; O, 4.66

Price and Availability

Size Price Availability Quantity
25mg USD 180 2 weeks
50mg USD 290 2 weeks
100mg USD 520 2 weeks
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Related CAS #: 24003-58-5 (QX-314 Br); 21306-56-9 (QX-314); 5369-03-9 (QX-314 HCl).  

Synonym: QX-314 Br; QX-314Br; QX314 Br; QX 314; QX314.

IUPAC/Chemical Name: N-(2,6-Dimethylphenylcarbamoylmethyl)triethylammonium bromide

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,6-8,12H2,1-5H3;1H

SMILES Code: CC[N+](CC)(CC(NC1=C(C)C=CC=C1C)=O)CC.[Br-]

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Biological target: QX 314 bromide is a sodium channel blocker.
In vitro activity: QX-314, a quaternary lidocaine derivative, has been shown to interact with and permeate TRPV1 channels to produce nociceptive and sensory blockade in animals in vivo. This study found that QX-314 activated TRPV1 channels at 10, 30, and 60 mM but not TRPV4 channels. This study shows that QX-314 exerts biphasic effects on TRPV1 channels, inhibiting capsaicin-evoked TRPV1 currents at lower concentrations and activating TRPV1 channels at higher concentrations. These findings may provide an explanation for the irritant properties of intrathecal QX-314 in mice in vivo. Reference: Anesthesiology. 2011 Jun;114(6):1425-34. https://pubmed.ncbi.nlm.nih.gov/21502857/
In vivo activity: The use of QX-314 has been proposed to achieve selective inhibition of nociceptors that express transient receptor potential vanilloid 1 (TRPV1) channels with fewer motor deficits. This study examined the effects of QX-314 on respiratory rhythm generation in brainstem-spinal cord preparations from newborn rats. The extracellular application of QX-314 decreased the C4 burst rate, amplitude, and slope during the initial rising phase. These findings could help explain one of the mechanisms underlying the central toxicities that occur after the systemic application of QX-314. Reference: Neurosci Lett. 2016 Apr 21;619:121-5. https://pubmed.ncbi.nlm.nih.gov/26992939/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Water 34.3 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 343.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Rivera-Acevedo RE, Pless SA, Ahern CA, Schwarz SK. 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. doi: 10.1097/ALN.0b013e318216ea0c. Erratum in: Anesthesiology. 2015 Aug;123(2):492. PMID: 21502857. 2. Armogida M, Giustizieri M, Zona C, Piccirilli S, Nisticò R, Mercuri NB. N-ethyl lidocaine (QX-314) protects striatal neurons against ischemia: an in vitro electrophysiological study. Synapse. 2010 Feb;64(2):161-8. doi: 10.1002/syn.20735. PMID: 19852070. 3. Takahashi K, Hayakawa C, Onimaru H. Effects of a quaternary lidocaine derivative, QX-314, on the respiratory activity in brainstem-spinal cord preparation from newborn rats. Neurosci Lett. 2016 Apr 21;619:121-5. doi: 10.1016/j.neulet.2016.03.022. Epub 2016 Mar 15. PMID: 26992939. 4. Perkins KL, Wong RK. Intracellular QX-314 blocks the hyperpolarization-activated inward current Iq in hippocampal CA1 pyramidal cells. J Neurophysiol. 1995 Feb;73(2):911-5. doi: 10.1152/jn.1995.73.2.911. PMID: 7760149.
In vitro protocol: 1. Rivera-Acevedo RE, Pless SA, Ahern CA, Schwarz SK. 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. doi: 10.1097/ALN.0b013e318216ea0c. Erratum in: Anesthesiology. 2015 Aug;123(2):492. PMID: 21502857. 2. Armogida M, Giustizieri M, Zona C, Piccirilli S, Nisticò R, Mercuri NB. N-ethyl lidocaine (QX-314) protects striatal neurons against ischemia: an in vitro electrophysiological study. Synapse. 2010 Feb;64(2):161-8. doi: 10.1002/syn.20735. PMID: 19852070.
In vivo protocol: 1. Takahashi K, Hayakawa C, Onimaru H. Effects of a quaternary lidocaine derivative, QX-314, on the respiratory activity in brainstem-spinal cord preparation from newborn rats. Neurosci Lett. 2016 Apr 21;619:121-5. doi: 10.1016/j.neulet.2016.03.022. Epub 2016 Mar 15. PMID: 26992939. 2. Perkins KL, Wong RK. Intracellular QX-314 blocks the hyperpolarization-activated inward current Iq in hippocampal CA1 pyramidal cells. J Neurophysiol. 1995 Feb;73(2):911-5. doi: 10.1152/jn.1995.73.2.911. PMID: 7760149.

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1. Talbot and Sayer (1996) Intracellular QX-314 inhibits calcium currents in hippocampal CA1 pyramidal neurons. J.Neurophysiol. 76 2120. PMID: 8890325.

2. Perkins and Wong (1995) Intracellular QX-314 blocks the hyperpolarization activated inward current Iq in hippocampal CA1 pyramidal cells. J.Neurophysiol. 73 911. PMID: 7760149.