| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Cardiac sodium channels (Class I antiarrhythmic mechanism); targets involved in myocardial membrane stabilization.
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| ln Vitro |
In vitro, Droxicainide decreases the excitability and contractility of the sinoatrial node and atria. As a sodium channel blocker, it reduces the rate of phase 0 depolarization in cardiac action potentials, thereby suppressing abnormal automaticity and reentrant arrhythmias. Quantitative in vitro electrophysiology data (e.g., IC50 for sodium channel block) is limited in publicly available literature.
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| ln Vivo |
Droxicainide decreased the extent of canine infarcts and areas of hypoperfusion that developed into necrosis in tests of coronary artery blockage [1]. Drosikanide decreased the excitability and contractility of the sinoatrial node, atria, and ventricles and increased refractoriness in rat investigations of spontaneously beating atria, electrical stimulation of the atria, and papillary muscles [2].
In vivo, Droxicainide decreases the extent of canine infarcts and areas of hypoperfusion that develop into necrosis in coronary artery occlusion models. It reduces the hypoperfused area that evolves to necrosis and reduces infarct size in dogs. These findings suggest cardioprotective effects in ischemic conditions. |
| Enzyme Assay |
No specific cell-free sodium channel binding assay protocol is detailed for Droxicainide. For sodium channel blockers, typical cell-free assays include radioligand binding studies using [3H]batrachotoxin or [3H]saxitoxin and purified sodium channel preparations, or electrophysiology using voltage-clamp techniques in heterologous expression systems.
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| Cell Assay |
Cellular electrophysiology is assessed in isolated cardiac myocytes or heterologous cells expressing cardiac sodium channels (e.g., HEK-293 cells expressing Nav1.5). Whole-cell patch-clamp recordings are performed to measure sodium current (INa) inhibition by Droxicainide. Cells are voltage-clamped, and sodium currents are elicited by depolarizing pulses; IC50 values are calculated from concentration-dependent inhibition curves.
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| Animal Protocol |
In vivo efficacy is evaluated in canine models of coronary artery occlusion. Dogs are anesthetized, and the coronary artery is ligated to induce ischemia. Droxicainide is administered intravenously. Endpoints include infarct size measurement (triphenyltetrazolium chloride staining), area of hypoperfusion (fluorescent microspheres), and hemodynamic parameters.
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| ADME/Pharmacokinetics |
Molecular weight: 276.37; molecular formula: C16H24N2O2. Purity: 98%. IUPAC name: N-(2,6-dimethylphenyl)-1-(2-hydroxyethyl)piperidine-2-carboxamide. Storage: typical for small-molecule compounds (desiccated, protected from light).
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a Class I antiarrhythmic agent, potential proarrhythmic effects (e.g., QT prolongation, torsades de pointes) would be a concern, similar to other sodium channel blockers. Standard toxicological studies would be required for drug development.
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| References |
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| Additional Infomation |
Droxicainide is a research-grade compound, not approved for therapeutic use in major markets. It has been studied as an antiarrhythmic agent for treating cardiac arrhythmias. No FDA approval or recent clinical trials have been reported. Its mechanism involves Class I sodium channel blockade.
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| Molecular Formula |
C16H24N2O2
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|---|---|
| Molecular Weight |
276.374
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| Exact Mass |
276.184
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| CAS # |
78289-26-6
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| PubChem CID |
157187
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.133g/cm3
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| Boiling Point |
456.2ºC at 760 mmHg
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| Flash Point |
229.7ºC
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| Index of Refraction |
1.578
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| LogP |
2.676
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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 |
4
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| Heavy Atom Count |
20
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| Complexity |
312
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1N(CCO)CCCC1)NC2=C(C)C=CC=C2C
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| InChi Key |
NVASAXNGHUPVJX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H24N2O2/c1-12-6-5-7-13(2)15(12)17-16(20)14-8-3-4-9-18(14)10-11-19/h5-7,14,19H,3-4,8-11H2,1-2H3,(H,17,20)
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| Chemical Name |
N-(2,6-dimethylphenyl)-1-(2-hydroxyethyl)piperidine-2-carboxamide
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6183 mL | 18.0917 mL | 36.1834 mL | |
| 5 mM | 0.7237 mL | 3.6183 mL | 7.2367 mL | |
| 10 mM | 0.3618 mL | 1.8092 mL | 3.6183 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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