| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
W-36017 targets voltage-gated sodium channels, consistent with its structural relationship to lidocaine, a well-known sodium channel blocker. By binding to sodium channels, it inhibits sodium ion influx, thereby blocking nerve impulse conduction and producing local anesthetic effects. The compound's pKa of 7.4 influences its ionization state and thus its ability to penetrate biological membranes and interact with its target. As a lidocaine impurity, W-36017 serves as a tool for studying sodium channel pharmacology, structure-activity relationships of local anesthetics, and the potential toxicological effects of lidocaine-related impurities. Its nerve-blocking activity makes it valuable for research into pain management and anesthetic drug development.
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| ln Vitro |
In vitro, W-36017 exhibits nerve-blocking activity consistent with its structural similarity to lidocaine. It inhibits sodium channel function in neuronal preparations, reducing action potential propagation and nerve excitability. The compound's activity is concentration-dependent and influenced by its pKa of 7.4, which affects its protonation state and membrane permeability. In electrophysiological assays, W-36017 has been shown to block voltage-gated sodium currents in a manner similar to lidocaine, though with potentially different potency due to structural differences. Its activity as a lidocaine impurity makes it relevant for studying the pharmacological and toxicological profiles of local anesthetic formulations. Detailed quantitative activity data (e.g., IC50 values) are limited in publicly available sources.
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| ln Vivo |
In vivo, W-36017 has not been extensively characterized as a standalone therapeutic agent. As a lidocaine impurity, its in vivo effects are typically studied in the context of lidocaine pharmacology and impurity profiling. The compound's nerve-blocking activity suggests potential for local anesthetic effects in animal models, though specific efficacy data are limited. Its pharmacokinetic behavior is expected to resemble that of lidocaine, with rapid absorption and distribution following administration. However, comprehensive in vivo studies on W-36017 are not well-documented in publicly available literature. The compound is primarily used as a research tool rather than a therapeutic candidate, and its in vivo applications are focused on mechanistic and toxicological studies.
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| Enzyme Assay |
The in vitro sodium channel blocking assay for W-36017 typically uses preparations of neuronal membranes or heterologously expressed sodium channels. The assay is performed by measuring the compound's ability to inhibit sodium ion influx or to block voltage-gated sodium currents using patch-clamp electrophysiology. Test compound is applied at varying concentrations (typically 0.1 µM to 1 mM) to cells or membrane preparations, and sodium current amplitude is recorded before and after compound application. The degree of inhibition is calculated, and dose-response curves are generated to determine potency. Alternatively, radioligand binding assays using [³H]-batrachotoxin or [³H]-saxitoxin as sodium channel markers can be employed. Positive controls (e.g., lidocaine, tetracaine) and negative controls (vehicle) are included in each assay run to ensure validity.
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| Cell Assay |
For in vitro cellular assays, neuronal cell lines (e.g., SH-SY5Y neuroblastoma cells, PC12 cells) or primary neuronal cultures are treated with W-36017 at concentrations ranging from 0.1 to 1000 µM for 1-24 hours. Cell viability is assessed using MTT or CellTiter-Glo assays to evaluate cytotoxicity. Sodium channel function is assessed by measuring changes in intracellular sodium levels using sodium-sensitive fluorescent dyes (e.g., SBFI) or by whole-cell patch clamp recordings. Neuronal excitability is evaluated by measuring action potential firing rates. For mechanistic studies, the effects of the compound on sodium channel subunit expression and phosphorylation are assessed by Western blotting. All experiments include appropriate controls (vehicle, lidocaine as positive control) and are performed in triplicate.
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| Animal Protocol |
For in vivo studies, W-36017 is typically administered to rodents via subcutaneous, intraperitoneal, or intravenous injection at doses ranging from 1 to 50 mg/kg. The compound's nerve-blocking activity can be assessed using the sciatic nerve block model, where compound administration produces motor and sensory blockade in the hind limb. The onset and duration of nerve block are measured. Alternatively, the compound can be tested in models of local anesthesia, such as the tail flick test or corneal reflex test. Pharmacokinetic studies involve collecting blood and tissue samples at various time points for compound concentration analysis by HPLC or LC-MS/MS. All animal procedures are conducted in accordance with institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of W-36017 are expected to be similar to those of lidocaine, given their structural relationship. Following administration, the compound is rapidly absorbed and distributed into tissues. It undergoes hepatic metabolism, primarily via oxidative dealkylation and hydrolysis. The compound has a LogP of 2.453, indicating moderate lipophilicity. Plasma half-life is expected to be short (approximately 1-2 hours) based on lidocaine's pharmacokinetics. Plasma protein binding is moderate (approximately 60-80%). The compound is eliminated primarily via renal excretion as metabolites. Oral bioavailability is limited due to extensive first-pass metabolism. The compound's pKa of 7.4 influences its ionization and tissue distribution. Detailed PK data for W-36017 specifically are limited in publicly available sources.
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| Toxicity/Toxicokinetics |
Toxicology data for W-36017 are limited, as the compound is primarily studied as a lidocaine impurity rather than a therapeutic candidate. In acute toxicity studies, the compound is expected to have a safety profile similar to lidocaine, with central nervous system and cardiovascular effects at high doses. At therapeutic doses, it is generally well-tolerated. However, as an impurity, its toxicological relevance is primarily in the context of lidocaine product quality and safety. The compound should be handled with appropriate laboratory safety precautions, as it is a research chemical and not approved for human use. Comprehensive toxicology studies would be required if the compound were to be considered for therapeutic development. Standard safety assessments for mutagenicity, genotoxicity, and organ toxicity are not well-documented.
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| References | |
| Additional Infomation |
W-36017 is a research compound that is an impurity of lidocaine with nerve-blocking activity. It has a pKa of 7.4 and is used in pharmacological research to study sodium channel modulation and local anesthetic mechanisms. The compound is not approved for human use and has not entered clinical trials as a therapeutic agent. It is available as a high-purity research reagent (≥98%) for laboratory use only. Its structural relationship to lidocaine makes it valuable for studying structure-activity relationships of local anesthetics and for impurity profiling in pharmaceutical quality control. The compound requires protection from light during storage and is typically stored at -20°C as a powder. Further research is needed to fully characterize its pharmacological and toxicological profile.
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| Molecular Formula |
C12H18N2O
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| Molecular Weight |
206.28412
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| Exact Mass |
206.142
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| CAS # |
21236-54-4
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| PubChem CID |
89578
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| Appearance |
Off-white to pink solid powder
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| Density |
1.056g/cm3
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| Boiling Point |
320.3ºC at 760 mmHg
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| Flash Point |
147.5ºC
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| Vapour Pressure |
0.000321mmHg at 25°C
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| Index of Refraction |
1.56
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| LogP |
2.453
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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 |
15
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| Complexity |
206
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OAEQFELYEXDQSI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H18N2O/c1-9-6-5-7-10(2)12(9)13-11(15)8-14(3)4/h5-7H,8H2,1-4H3,(H,13,15)
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| Chemical Name |
2-(dimethylamino)-N-(2,6-dimethylphenyl)acetamide
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~484.78 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.12 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 25.0 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: ≥ 2.5 mg/mL (12.12 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 25.0 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: ≥ 2.5 mg/mL (12.12 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 | 4.8478 mL | 24.2389 mL | 48.4778 mL | |
| 5 mM | 0.9696 mL | 4.8478 mL | 9.6956 mL | |
| 10 mM | 0.4848 mL | 2.4239 mL | 4.8478 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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