QX-314 (bromide)

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.Formal Name: 2-[(2,6-dimethylphenyl)amino]-N,N,N-triethyl-2-oxo-ethanaminium bromide. CAS Number: 24003-58-5. Molecular Formula: C16H27N2O . Br. Formula Weight: 343.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 20 mg/ml, Ethanol: 2 mg/ml, PBS (pH 7.2): 10 mg/ml. SMILES: CC[N](CC)(CC)CC(=O)Nc1c(C)cccc1C. 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. InChi Key: DLHMKHREUTXMCH-UHFFFAOYSA-N.