| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
The compound primarily acts as a sodium channel blocker. Its antitussive effect is mediated through inhibition of airway sensory nerve discharges, particularly rapidly adapting stretch receptors (RARs). It may also interact with transient receptor potential (TRP) channels involved in sensory nerve activation during coughing. Unlike lidocaine, its mechanism is distinct and does not involve general local anesthesia. The compound's mechanism of action is distinct from that of lidocaine, suggesting a unique therapeutic profile.
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| ln Vitro |
Carcainium chloride demonstrates significant antitussive activity in preclinical studies. It inhibits discharges in airway sensory nerves, reducing the cough reflex. The compound's activity is assessed by measuring its ability to suppress cough responses in animal models and to inhibit sensory nerve firing in isolated nerve preparations. The compound exhibits significant antitussive activity, making it useful in the study of cough mechanisms.
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| ln Vivo |
A pilot study involving eight female patients (mean age 71 years) with IIP demonstrated that nebulized carcainium chloride significantly reduced cough frequency and improved quality of life without significant side effects. The study employed a double-blind, randomized, placebo-controlled crossover design. No adverse events were reported during the study, nor were any changes in ECG variables, spirometry, urine and blood tests noted. The results indicate that nebulized VRP700 improved cough and quality of life in hospitalized IIP patients with no significant side effects.
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| Enzyme Assay |
Carcainium chloride's sodium channel blocking activity can be assessed using electrophysiological patch-clamp techniques on isolated sensory neurons or heterologously expressed sodium channels. Inhibition of sensory nerve firing can be evaluated using ex vivo nerve recording preparations from airway tissues.
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| Cell Assay |
Cellular activity of carcainium chloride can be evaluated in neuronal cell lines or primary sensory neurons using patch-clamp electrophysiology to measure sodium channel inhibition. Calcium imaging may also be used to assess neuronal excitability changes in response to compound treatment.
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| Animal Protocol |
In vivo antitussive activity is evaluated in animal models of cough, such as guinea pigs or cats, where cough reflexes are induced by chemical or mechanical stimulation. The compound is typically administered via nebulization, and cough frequency is quantified to determine the antitussive effect.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for carcainium chloride are limited. As a quaternary ammonium compound, it is expected to have poor oral bioavailability and is typically administered via inhalation for local action in the airways. Systemic absorption following inhalation is likely minimal. The compound is administered as an aerosol (VRP700).
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| Toxicity/Toxicokinetics |
No comprehensive toxicity data have been reported for carcainium chloride. In the pilot study in IIP patients, nebulized administration was well tolerated without significant side effects. As a quaternary ammonium compound, it is expected to have low systemic toxicity due to limited absorption. No adverse events were reported.
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| References | |
| Additional Infomation |
Lidocaine derivatives with antiarrhythmic activity; structure
Carcainium chloride is a research compound not approved for clinical use. It has been investigated as a potential therapeutic for chronic cough, particularly in patients with idiopathic interstitial pneumonias. Its mechanism of action is distinct from conventional cough suppressants, making it a valuable tool for studying cough reflex pathways and developing novel antitussive therapies. The compound is also known as VRP700 in clinical studies. It is for research use only. |
| Molecular Formula |
C18H22CLN3O2
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|---|---|
| Molecular Weight |
347.84
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| Exact Mass |
347.14
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| CAS # |
1042-42-8
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| PubChem CID |
13966
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
361
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C[N+](C)(CC(=O)NC1=CC=CC=C1)CC(=O)NC2=CC=CC=C2.[Cl-]
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| InChi Key |
YGCONRRHHMKQRL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H21N3O2.ClH/c1-21(2,13-17(22)19-15-9-5-3-6-10-15)14-18(23)20-16-11-7-4-8-12-16;/h3-12H,13-14H2,1-2H3,(H-,19,20,22,23);1H
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| Chemical Name |
bis(2-anilino-2-oxoethyl)-dimethylazanium;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 (e.g. under nitrogen), 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: 33.33 mg/mL (95.82 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (2.39 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 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 0.83 mg/mL (2.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 8.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8749 mL | 14.3744 mL | 28.7489 mL | |
| 5 mM | 0.5750 mL | 2.8749 mL | 5.7498 mL | |
| 10 mM | 0.2875 mL | 1.4374 mL | 2.8749 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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