QX-314 |
| Catalog No.GC13781 |
QX-314 est un bloqueur de canaux sodiques chargé en permanence et imperméable À la membrane.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 24003-58-5
Sample solution is provided at 25 µL, 10mM.
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QX-314 is a positively charged, membrane-impermeable quaternary lidocaine derivative [1][2][3][4].
QX-314 is a local anesthetic. In CAl pyramidal neurons of the guinea-pig hippocampal slice, QX-314 blocked both Na+ dependent action potentials and the voltage-dependent, non-inactivating Na+ conductance [1]. In Xenopus laevis oocytes expressed TRPV1 and TRPV4 channels, QX-314 (10, 30, and 60 mM) activated TRPV1 channels, but not TRPV4 channels. QX-314 at lower concentrations (less than 1mM) potently inhibited capsaicin-evoked TRPV1 currents with IC50 value of 8.0 μM. In TRPV1-expressing tsA201 cells, QX-314 induced transient increase in cytoplasmic Ca2+ [2]. In large-diameter human DRG neurons, flagellin/QX-314 inhibited sodium currents [3].
In three standard local anesthetic animal models, QX-314 reversibly and concentration-dependently induced long-lasting local anesthesia with a slow onset [4]. Intraplantar co-application of flagellin/QX-314 inhibited mechanical allodynia after nerve injury, chemotherapy and diabetic neuropathy in a dose-dependent way. In naive and chemotherapy-treated mice, co-application of flagellin/QX-314 selectively inhibited Aβ-fiber conduction [3].
References:
[1]. Connors BW, Prince DA. Effects of local anesthetic QX-314 on the membrane properties of hippocampal pyramidal neurons. J Pharmacol Exp Ther, 1982, 220(3): 476-481.
[2]. 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, 114(6): 1425-1434.
[3]. Xu ZZ, Kim YH, Bang S, et al. Inhibition of mechanical allodynia in neuropathic pain by TLR5-mediated A-fiber blockade. Nat Med, 2015, 21(11): 1326-1331.
[4]. Lim TK, Macleod BA, Ries CR, et al. The quaternary lidocaine derivative, QX-314, produces long-lasting local anesthesia in animal models in vivo. Anesthesiology, 2007, 107(2): 305-311.
| Cas No. | 24003-58-5 | SDF | |
| Chemical Name | 2-((2,6-dimethylphenyl)amino)-N,N,N-triethyl-2-oxoethanaminium bromide | ||
| Canonical SMILES | CC1=CC=CC(C)=C1N([H])C(C[N+](CC)(CC)CC)=O.[Br-] | ||
| Formula | C16H27BrN2O | M.Wt | 343.3 |
| Solubility | 5 mg/ml in DMF; 20 mg/ml in DMSO; 2 mg/ml in Ethanol; 10 mg/ml in PBS (pH 7.2). | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9129 mL | 14.5645 mL | 29.129 mL |
| 5 mM | 0.5826 mL | 2.9129 mL | 5.8258 mL |
| 10 mM | 0.2913 mL | 1.4565 mL | 2.9129 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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