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QX-314 (bromide) (CAS 24003-58-5) LS-H53

TRPV1 receptor agonist
LS-H53-25 / 25 mg / $175
LS-H53-50 / 50 mg / $185
LS-H53-100 / 100 mg / $205
USA Shipment Only
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Description: QX-314 is a membrane-impermeant lidocaine derivative that selectively blocks sodium channels on nociceptive neurons when delivered intracellularly via the TRPV1 channel, but is reportedly ineffective with extracellular application. When supplied in combination with 1 µM capsaicin, a TRPV1 receptor agonist, 5 mM QX-314 blocks 98% of sodium current in voltage-clamped nociceptive DRG neurons. QX-314 elicits a long-lasting decrease in the response to painful mechanical and thermal stimuli without imparting the motor deficits (e.g., numbness, paralysis) associated with many conventional local anesthetics. At concentrations ranging from 10-70 mM, peripheral application of QX-314 dose-dependently produces robust local anesthesia with slow onset in the guinea pig intradermal wheal assay, the murine tail-flick test, and the murine sciatic nerve blockade model. However, injection of 0.5-30 mM QX-314 in the lumbar intrathecal space produces neurotoxicity and death in mice. H53_ChemicalStructureImage.png
2-[(2,6-dimethylphenyl)amino]-N,N,N-triethyl-2-oxo-ethanaminium bromide
 
biochemical, chemical, agonist
LS-H53
24003-58-5
C16H27N2O · Br
≥98%
A crystalline solid
0
CC[N](CC)(CC)CC(=O)Nc1c(C)cccc1C
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
DLHMKHREUTXMCH-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: VR1 / TRPV1 related products

Usage Information

QX-314 (bromide) is supplied as a crystalline solid. A stock solution may be made by dissolving the QX-314 (bromide) in an organic solvent purged with an inert gas. QX-314 (bromide) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide. The solubility of QX-314 (bromide) in these solvents is approximately 2, 20, and 5 mg/ml, respectively. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of QX-314 (bromide) can be prepared by directly dissolving the crystalline compound in aqueous buffers. The solubility of QX-314 (bromide) in PBS, pH 7.2, is approximately 10 mg/ml. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Binshtok, A.M., Bean, B.P., and Woolf, C.J. Inhibition of nociceptors by TRPV1-mediated entry of impermeant sodium channel blockers. Nature 449, 607-610 (2007).
  2. Lim, T.K.Y., MacLeod, B.A., Ries, C.R., et al. The quaternary lidocaine derivative, QX-314, produces longlasting local anesthesia in animal models in vivo. Anesthesiology 107, 305-311 (2007).
  3. Schwarz, S., Cheung, H., Ries, C., et al. 473931-Lumbar intrathecal administration of the quaternary lidocaine derivative, QX-314, produces neurotoxicity in mice. Anesthesiology 107, 305-311 (2008).

 


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