| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Voltage-gated Sodium Channels (NaV)
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|---|---|
| ln Vitro |
As compared to μ1-WT, μ1 IP-Loop to Heart Sequence (μ1-Y401C) exhibits a considerable block twelve minutes after the external administration of 500 μM QX222 chloride (WT, 14.2±1.6% block, n = 8; Y401C, 45.2± 3.6% block, n = 9; P < 0.001)[1].
QX-222 chloride is a trimethyl analog of lignocaine and a potent Na+ channel blocker. Its quaternary ammonium structure makes it membrane-impermeant, enabling selective block of sodium channels from the intracellular side. This property allows researchers to study channel gating, neuronal excitability, and action potential propagation by applying the drug to the inside of cells via patch pipettes. |
| ln Vivo |
In sham-operated rats, QX-222 (10 mg/kg; intravenous infusion; 7 days) chloride reverses the heat hypersensitivity caused by spinal nerve ligation (SNL) and induces antinociception[2].
In vivo, QX-222 chloride (administered intravenously) has been shown to reverse spinal nerve ligation (SNL)-induced thermal hypersensitivity, indicating potential for neuropathic pain studies. |
| Enzyme Assay |
For intracellular application, QX-222 chloride is included in the patch pipette solution during whole-cell patch-clamp recordings. The internal solution typically contains QX-222 at concentrations of 0.1-5 mM. After establishing whole-cell configuration, the compound diffuses into the cell and blocks sodium channels from the intracellular side. For in vitro nerve studies, isolated nerves are placed in a recording chamber and QX-222 is applied to the axoplasm via microinjection or cut-end loading. Sodium currents are measured before and after QX-222 application.
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| Cell Assay |
For patch-clamp studies, cells (e.g., HEK293 cells expressing NaV channels or cultured neurons) are plated on coverslips. The internal pipette solution contains QX-222 chloride (0.1-5 mM). After establishing whole-cell configuration, the cell is dialyzed with the internal solution. Sodium currents are recorded using a holding potential of -120 mV with depolarizing steps to -10 mV. The block of sodium current is assessed over time as QX-222 diffuses into the cell.
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| Animal Protocol |
In a rodent model of neuropathic pain, male Sprague-Dawley rats are subjected to spinal nerve ligation (SNL) at the L5 and L6 spinal nerves. After recovery (7 days), rats are tested for thermal hypersensitivity using a Hargreaves apparatus. QX-222 chloride is administered intravenously (dose not specified) and paw withdrawal latency is measured. QX-222 reverses SNL-induced thermal hypersensitivity, indicating an analgesic effect.
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| ADME/Pharmacokinetics |
No specific PK data for QX-222 chloride. As a charged quaternary ammonium compound, it is poorly absorbed orally and does not cross the blood-brain barrier. For in vivo studies, it is typically administered intravenously. Its membrane-impermeant nature means it acts from the extracellular (or intracellular) side depending on application, limiting systemic distribution.
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| Toxicity/Toxicokinetics |
No specific toxicity data for QX-222 chloride. As a quaternary lidocaine derivative, it is generally less toxic than its tertiary amine counterparts due to reduced CNS penetration. For research use, handle with standard laboratory precautions (gloves, lab coat, eye protection). Toxicity studies would be required for therapeutic development.
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| References |
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| Additional Infomation |
QX-222 chloride (CAS: 5369-00-6) is a research tool for studying voltage-gated sodium channels in neurophysiology. Its charged, membrane-impermeant structure makes it unique for selectively blocking channels from the inside, helping to map drug-binding sites on the channel pore. QX-222 is not approved for human use. References: Strichartz GR. J Gen Physiol. 1973;62(1):37-57.
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| Molecular Formula |
C13H21CLN2O
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|---|---|
| Molecular Weight |
256.77
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| Exact Mass |
256.134
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| CAS # |
5369-00-6
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| PubChem CID |
9795082
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| Appearance |
White to off-white solid powder
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| LogP |
3.272
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
17
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| Complexity |
235
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C(=CC=C1)C)NC(=O)C[N+](C)(C)C.[Cl-]
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| InChi Key |
WFKXSWWTOZBDME-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H20N2O.ClH/c1-10-7-6-8-11(2)13(10)14-12(16)9-15(3,4)5;/h6-8H,9H2,1-5H3;1H
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| Chemical Name |
[2-(2,6-dimethylanilino)-2-oxoethyl]-trimethylazanium;chloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 125 mg/mL (486.82 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8945 mL | 19.4727 mL | 38.9454 mL | |
| 5 mM | 0.7789 mL | 3.8945 mL | 7.7891 mL | |
| 10 mM | 0.3895 mL | 1.9473 mL | 3.8945 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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