QX-314
目录号 : GC13781A selective sodium channel blocker
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 | |
| 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 | 0.5826 mL | 2.9129 mL | 5.8258 mL |
| 10 mM | 0.2913 mL | 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet