Size | Price | Stock | Qty |
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500mg |
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1g |
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5g |
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10g |
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25g |
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Other Sizes |
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Lidocaine hydrochloride monohydrate (also known as Alphacaine; Lignocaine) is a potent and selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Lidocaine is a local anesthetic and cardiac depressant used as an antiarrhythmia agent. Originally developed as a local anesthetic, it has properties as a class IB antiarrhythmic, a long-acting membrane stabilizing agent used against ventricular arrhythmia. Its actions are more intense and its effects more prolonged than those of procaine but its duration of action is shorter than that of bupivacine or prilocaine.
ln Vitro |
Lidocaine hydrochloride (10 nM; 48 hours) greatly decreases cell proliferation [2]. Lidocaine hydrochloride (1-10 nM; 24-72 hours) decreases cell viability, attaining the highest inhibitory impact at a concentration of 10 nM and 48 treatment times [2] Lidocaine hydrochloride (10 nM; 48 hours) dramatically increases cell viability. Sterilization rate[2]. Lidocaine hydrochloride (10 nM; 48 hours) suppresses cyclin D1 and dramatically upregulates p21 expression [2].
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ln Vivo |
In the stent, lidocaine hydrochloride causes a total reverse tail nerve block. The mechanical pain blockade caused by lidocaine hydrochloride had a shorter onset and quicker recovery than thermal pain blockade [3].
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Cell Assay |
Cell proliferation analysis[2].
Cell Types: human gastric cancer cell line MKN45 Tested Concentrations: 10 nM Incubation Duration: 48 hrs (hours) Experimental Results: Cell proliferation diminished Dramatically. Cell viability assay [2] Cell Types: human gastric cancer cell line MKN45 Tested Concentrations: 1, 5 and 10 nM Incubation Duration: 24, 48, 72 hrs (hours) Experimental Results: Inhibition of MKN45 cell viability. Cell apoptosis analysis [2] Cell Types: Human gastric cancer cell line MKN45 Tested Concentrations: 10 nM Incubation Duration: 48 hrs (hours) Experimental Results: The cell apoptosis rate increased Dramatically. Western Blot Analysis [2] Cell Types: human gastric cancer cell line MKN45 Tested Concentrations: 10 nM Incubation Duration: 48 hrs (hours) Experimental Results: Cyclin D1 expression was Dramatically down-regulated, and p21 expression was Dramatically up-regulated. |
References |
[1]. Cummins TR, et al. Setting up for the block: the mechanism underlying lidocaine's use-dependent inhibition of sodium channels. J Physiol. 2007 Jul 1;582(Pt 1):11.
[2]. Sui H, et al. Lidocaine inhibits growth, migration and invasion of gastric carcinoma cells by up-regulation of miR-145. BMC Cancer. 2019 Mar 15;19(1):233. [3]. Li Z, et al. Evaluation of the antinociceptive effects of lidocaine and bupivacaine on the tail nerves of healthy rats. Basic Clin Pharmacol Toxicol. 2013 Jul;113(1):31-6. |
Molecular Formula |
C₁₄H₂₃CLN₂O
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Molecular Weight |
270.80
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CAS # |
73-78-9
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Related CAS # |
Lidocaine;137-58-6;Lidocaine-d6 hydrochloride;2517378-96-8;Lidocaine-d10 hydrochloride;1189959-13-4;Lidocaine;137-58-6
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SMILES |
O=C(NC1=C(C)C=CC=C1C)CN(CC)CC.[H]Cl
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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) |
H2O : ≥ 100 mg/mL (~369.28 mM)
DMSO : ≥ 100 mg/mL (~369.28 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.23 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 (9.23 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 (9.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 120 mg/mL (443.13 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.6928 mL | 18.4638 mL | 36.9276 mL | |
5 mM | 0.7386 mL | 3.6928 mL | 7.3855 mL | |
10 mM | 0.3693 mL | 1.8464 mL | 3.6928 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.