Lidocaine (Synonyms: NSC 40030) |
Catalog No.GC17608 |
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Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 137-58-6
Sample solution is provided at 25 µL, 10mM.
Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is a commonly used local anesthetics of amide derivative, a drug to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
Lidocaine (Lignocaine) (10 nM; 48 hours) decreases significantly cell proliferation[2]. Lidocaine (1-10 nM; 24-72 hours) inhibits cell viability and achieves the most suppressing effects at the concentration of 10 nM and treatment time 48 hours[2]. Lidocaine (10 nM; 48 hours) increases significantly the apoptotic cell rate[2]. Lidocaine (10 nM; 48 hours) down-regulates Cyclin D1 and up-regulates p21 expression significantly[2].
Lidocaine (Lignocaine) causes completely reversible tail nerve block in rats. Mechanical nociception block produced by lidocaine has slower onset and faster recovery compared with thermal nociception block[3].
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.
Cell experiment [1,2]: | |
Cell lines |
Fresh bovine articular chondrocytes, sarcoplasmic reticulum |
Preparation method |
The solubility of this compound in DMSO is >11.7 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition |
1% or 2% lidocaine, 30 minutes |
Applications |
Lidocaine (1%, 15-minute) decreased chondrocyte viability. Longer exposures to 1% and 2% lidocaine further reduced chondrocyte viability. Lidocaine (40 μM) showed reverse frequency-dependent depression of myocardial contractility. Lidocaine(40 μM, 100 μM) caused a marked depression of the late-peaking contractile responses, attributed to Ca2+ release from the sarcoplasmic reticulum. |
Animal experiment [3]: | |
Animal models |
Dogs with 2-hour-old myocardial infarctions |
Dosage form |
Intravenous bolus injection, 2-8 μg/ml |
Application |
Lidocaine prolonged the Q-EG intervals in the infarcted zones of the heart 17-26% at peak effect, but it had no effect on the Q-EG intervals in the normal zone except for a slight (1.5%) prolongation shortly after the initial intravenous bolus injection. Lidocaine prolonged the effective refractory period of the infarcted zone 23% at peak effect but had no effect on the effective refractory period of the normal zone. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Karpie J C, Chu C R. Lidocaine exhibits dose-and time-dependent cytotoxic effects on bovine articular chondrocytes in vitro[J]. The American journal of sports medicine, 2007, 35(10): 1622-1627. [2]. Lynch III C. Depression of myocardial contractility in vitro by bupivacaine, etidocaine, and lidocaine[J]. Anesthesia & Analgesia, 1986, 65(6): 551-559. [3]. Kupersmith J, Antman E M, Hoffman B F. In vivo electrophysiological effects of lidocaine in canine acute myocardial infarction[J]. Circulation research, 1975, 36(1): 84-91. |
Cas No. | 137-58-6 | SDF | |
Synonyms | NSC 40030 | ||
Chemical Name | 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide | ||
Canonical SMILES | CCN(CC)CC(=O)NC1=C(C=CC=C1C)C | ||
Formula | C14H22N2O | M.Wt | 234.34 |
Solubility | ≥ 11.7mg/mL in DMSO, ≥ 227.27mg/mL in EtOH | Storage | 4°C, protect from light |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 4.2673 mL | 21.3365 mL | 42.673 mL |
5 mM | 0.8535 mL | 4.2673 mL | 8.5346 mL |
10 mM | 0.4267 mL | 2.1337 mL | 4.2673 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5
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