QX-314 bromide
目录号 : GC13781QX-314 bromide是一种带正电、膜不透性的钠离子通道阻断剂。
Cas No.:24003-58-5
Sample solution is provided at 25 µL, 10mM.
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QX-314 bromide is a positively charged, membrane impermeable sodium ion channel blocker [1]. QX-314 bromide is a tetravalent lidocaine derivative that can specifically block sodium channels on pain-sensing neurons through the transient receptor potential vanilloid 1 (TRPV1) channel within cells [2-3]. QX-314 bromide can be used for local anesthesia [4].
In vitro, different concentrations of QX-314 bromide (1-1000μM) dose-dependently inhibit the voltage-gated sodium ion current (INa) of GH3 pituitary tumor cells, with a transient depolarization step causing a decrease in INa(T) amplitude and an enhanced inactivation phenomenon [5]. QX-314 bromide (15, 50, 100mM; 0-240min) reduces the cell viability of PC12 cells in a time- and dose-dependent manner, with lower cytotoxicity at 15 mM concentrations (cell viability > 75%) at all time points, and good cell viability at 100mM concentrations at 30 and 60 minutes (84.9% and 67.1%, respectively) [6].
In vivo, QX-314 bromide (15, 25, 50, and 100mM; corneal local administration, 30μL) dose-dependently increases the duration of anesthesia in rats, without significantly inhibiting corneal healing [6]. The combined treatment with QX-314 bromide (0.2%, 10μl, 1.6mg/kg/day; single-dose; intraplantar injections) and capsaicin can eliminate the responses of mice to harmful mechanical and thermal stimuli, significantly but temporarily increasing the thermal latency period, and does not cause motor or tactile defects [7].
References:
[1] Rivera-Acevedo RE, Pless SA, Ahern CA. 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.
[2] Binshtok A M, Bean B P, Woolf C J. Inhibition of nociceptors by TRPV1-mediated entry of impermeant sodium channel blockers[J]. Nature, 2007, 449(7162): 607-610.
[3] Puopolo M, Binshtok A M, Yao G L, et al. Permeation and block of TRPV1 channels by the cationic lidocaine derivative QX-314[J]. Journal of neurophysiology, 2013, 109(7): 1704-1712.
[4] Zhang Y J, Yang J, Yin Q Q, et al. QX-OH, a QX-314 derivative agent, produces long-acting local anesthesia in rats[J]. European Journal of Pharmaceutical Sciences, 2017, 105: 212-218.
[5] Wang J C F, Hsiao H T, Wu S N. Modulation of I Na, I h, and IK (erg) by Extracellular or Intracellular QX-314 (N-(2, 6-dimethylphenylcarbamoylmethyl) triethylammonium bromide) in Pituitary Tumor Cells[J]. International Journal of Molecular Sciences, 2025, 26(17): 8469.
[6] Woodruff A G, Santamaria C M, Mehta M, et al. Prolonged duration topical corneal anesthesia with the cationic lidocaine derivative QX-314[J]. Translational Vision Science & Technology, 2019, 8(5): 28-28.
[7] Binshtok AM, Gerner P, Oh SB, et al. Coapplication of lidocaine and the permanently charged sodium channel blocker QX-314 produces a long-lasting nociceptive blockade in rodents. Anesthesiology. 2009;111(1):127-137.
QX-314 bromide是一种带正电、膜不透性的钠离子通道阻断剂 [1]。QX-314 bromide是一种四价利多卡因衍生物，能够通过瞬时受体电位vanilloid 1（TRPV1）通道在细胞内特异性地阻断痛觉神经元上的钠通道 [2-3]。QX-314 bromide可用于局部麻醉 [4]。。
在体外，不同浓度的QX-314 bromide（1-1000μM）对GH3垂体瘤细胞的电压门控钠离子电流（INa）发生剂量依赖性抑制，短暂的去极化步骤引起INa(T)振幅降低，而其失活现象则有所增强 [5]。QX-314 bromide（15, 50, 100mM; 0-240min）以时间和剂量依赖性方式降低了PC12细胞的细胞活力，在15mM浓度下各时间细胞毒性低（细胞活力＞75%），在100mM浓度下30分钟和60分钟时也具有良好的细胞活力（84.9%和67.1%）[6]。
在体内，QX-314 bromide（15, 25, 50和100mM; 角膜局部给药, 30μL）剂量依赖性地增加了大鼠的麻醉持续时间，并且没有显著抑制角膜愈合 [6]。QX-314 bromide（0.2%, 10μl, 1.6mg/kg/day; 单剂量; 皮内注射）与辣椒素共处理可消除小鼠对有害机械和热刺激的反应，显著但短暂增长了热潜伏期，且不会导致运动或触觉缺陷 [7]。
| Cell experiment [1]: | |
Cell lines | PC12 cells |
Preparation Method | PC12 cells were plated and grown until 80% confluent in proliferation media composed of Dulbecco's modified Eagle's media (DMEM) supplemented with 12.5% horse serum and 2.5% fetal bovine serum. QX-314 bromide was prepared at various concentrations in 0.9% sterile saline. Drug solutions were prepared within 2 hours of use. For cell viability experiments, drugs were diluted to the appropriate concentration in DMEM cell media. We exposed cells to drug conditions for predetermined durations. Each condition (drug concentration and duration of exposure) including controls were performed in N = 18 replicate wells. Colorimetric absorbance at 490nm light was measured after 30, 60, 120, and 240 minutes for the MTS colorimetric assay. |
Reaction Conditions | 15, 50, 100mM; 0-240min |
Applications | The QX-314 bromide treatment reduced the cell viability of PC12 cells in a time- and dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Rats were gently towel restrained and received 30μL of either 15 or 100mM QX-314 bromide concentration on one eye. On the contralateral eye we applied either vehicle (0.9% NaCl) in a similar fashion (n = 5 eyes per condition with four total conditions, total of 10 animals). This was done hourly for 12 hours. After 15 seconds, the eye was gently closed to spread drug over the cornea. Every 15 minutes after drug administration, the eye was probed with a Cochet-Bonnet esthesiometer filament with the animal under gentle towel restraint. This filament is adjustable between 6 and 0.5cm, with shorter filament lengths providing a more noxious stimulus. Animals were then euthanized with carbon dioxide. Five additional animals who had received no treatments were also euthanized to serve as negative controls. Intact whole eyes were harvested for histologic analysis and fixed in 10% neutral buffered formalin. Hematoxylin and eosin staining and periodic acid-Schiff staining were performed on paraffin-embedded corneal sections and were evaluated qualitatively for evidence of epithelial, stromal, and endothelial changes. |
Dosage form | 15, 25, 50 and 100mM; local ocular administration, single dose, 30μL |
Applications | The QX-314 bromide treatment dose-dependently prolonged the anesthesia duration in rats, and did not significantly inhibit corneal healing. |
References: | |
| Cas No. | 24003-58-5 | SDF | |
| 化学名 | 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-] | ||
| 分子式 | C16H27BrN2O | 分子量 | 343.30 |
| 溶解度 | 5 mg/ml in DMF; 20 mg/ml in DMSO; 2 mg/ml in Ethanol; 10 mg/ml in PBS (pH 7.2). | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9129 mL | 14.5645 mL | 29.129 mL |
| 5 mM | 582.6 μL | 2.9129 mL | 5.8258 mL |
| 10 mM | 291.3 μL | 1.4565 mL | 2.9129 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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