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Lidocaine
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Catalog No. T0468Cas No. 137-58-6
Alias Xylocaine, Lignocaine, Alphacaine
Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammatory cytokines, and reduction of neutrophils influx.
Lidocaine
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Purity: 99.95%
Catalog No. T0468Alias Xylocaine, Lignocaine, AlphacaineCas No. 137-58-6
Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammatory cytokines, and reduction of neutrophils influx.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 500 mg | $45 | In Stock | In Stock |
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Purity:99.95%
Appearance:Solid
Color:White
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Product Introduction
Lidocaine AI Summary
Lidocaine exhibits diverse bioactivities and pharmacokinetic properties indicative of its potential therapeutic applications. It shows significant antiarrhythmic effects, demonstrated by its ability to reduce induced ventricular tachycardia (VT) and prolong the ventricular effective refractory period in various animal models, including dogs and guinea pigs. The compound affects cardiac electrophysiology by modulating the action potential duration and refractory period in canine Purkinje fibers and isolated right atria. Additionally, it impacts mean blood pressure during arrhythmias and has demonstrated local anesthetic activity in multiple assays, including in rat sciatic nerve models.
Pharmacokinetically, Lidocaine has an observed volume of distribution of 1.1 L/kg and an unbound plasma fraction of 0.3, suggesting moderate tissue distribution. It also shows a moderate octanol-water partition coefficient with log P values around 2.26 and variable permeability across different biological membranes, indicating balanced lipophilicity and potential for systemic absorption. The compound demonstrates efficient renal and hepatic clearance, with a total body clearance of 16.0 mL/min/kg.
Notably, Lidocaine exhibits inhibitory activity against several enzymes and receptors, including various voltage-gated sodium channels and calcium channels, which are crucial for its cardiac effects. It also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase at micromolar concentrations. The compound's interaction with neuronal sodium channels and ability to modulate Nav1.4, Nav1.7, and Nav1.3 channels further underscore its broad-spectrum bioactivity.
On the toxicity front, Lidocaine displays CNS toxicity in mice at higher doses, leading to ataxia and convulsions, and has an LD50 of 238.0 mg/kg, suggesting a narrow therapeutic window. However, the compound shows no significant hepatotoxicity, according to DILIps prediction scores. Its aqueous solubility (Log S value of -1.71) and intrinsic solubility of 3130.0 ug/mL imply moderate solubility, which is beneficial for formulation purposes.
Overall, Lidocaine demonstrates a comprehensive bioactivity profile suitable for developing antiarrhythmic and anesthetic therapies, with a need for careful dosing to mitigate potential CNS toxicities and optimize therapeutic efficacy..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammatory cytokines, and reduction of neutrophils influx. |
| Targets&IC50 | H1 receptor:>32 μM |
| Synonyms | Xylocaine, Lignocaine, Alphacaine |
| Molecular Weight | 234.34 |
| Formula | C14H22N2O |
| Cas No. | 137-58-6 |
| Smiles | N(C(CN(CC)CC)=O)C1=C(C)C=CC=C1C |
| Relative Density. | 1.026g/cm3 |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 250 mg/mL (1066.83 mM), Sonication is recommended.  H2O: 21.34 mM, Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (8.53 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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