Lidocaine
Based on 23 publication(s) in Google Scholar
Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence. 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 an amide derivative and has potential for the research of ventricular arrhythmia.
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- Pureza : 99.96%
- No. CAS: 137-58-6
- Fòrmula: C14H22N2O
- Peso molecular:234.34
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Lidocaine
More- Nat Methods. 2021 Jul;18(7):788-798. [Abstract]
- Nat Commun. 2026 Feb 10;17(1):2559. [Abstract]
- Sci Adv. 2026 Mar 6;12(10):eadw0891. [Abstract]
- Sci Adv. 2025 Dec 5;11(49):eadw7972. [Abstract]
- J Neuroinflammation. 2017 Nov 2;14(1):211. [Abstract]
- Stem Cell Res Ther. 2021 Feb 4;12(1):107. [Abstract]
- Transl Psychiatry. 2025 May 17;15(1):172. [Abstract]
- J Ethnopharmacol. 2025 May 12:347:119803. [Abstract]
- Biomater Adv. 2026 Jan:178:214452. [Abstract]
- Drug Des Devel Ther. 2024 Apr 9:18:1103-1114. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Int Immunopharmacol. 2023 Feb:115:109706. [Abstract]
- Mol Med Rep. 2022 May;25(5):150. [Abstract]
- PLoS Pathog. 2023 Feb 3;19(2):e1011126. [Abstract]
- Phytochemistry. 2026 Aug:248:114929. [Abstract]
- Reprod Toxicol. 2025 May:134:108895. [Abstract]
- Eur Spine J. 2022 Nov;31(11):2960-2971. [Abstract]
- J Phys D Appl Phys. 2019 Aug; 52(46).
- Neurogastroenterol Motil. 2023 Nov;35(11):e14677. [Abstract]
- PLoS One. 2025 Nov 4;20(11):e0335932. [Abstract]
- Dig Dis Sci. 2021 Dec;66(12):4384-4397. [Abstract]
- Eng Proc. 2026 Jan 14;110(1):7.
- University of Glasgow. 2023.
Customer Validation & Images
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RT-PCR
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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Cell Imaging/Staining
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Cell Imaging/Staining
Ver todos los productos específicos de isoformas MEK
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Actividad biológica
Descripciòn
IC50 & Target
[1,2]|
MEK |
ERK |
NF-κB |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>500 μM
Compound: lidocaine
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Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
180 μM
Compound: 1
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Inhibition of human TREK-1 expressed in HEK293 cells by patch-clamp technique
Inhibition of human TREK-1 expressed in HEK293 cells by patch-clamp technique
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[PMID: 23121096] |
| HEK293 | IC50 |
207 μM
Compound: 35
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Inhibition of of human TREK1 expressed in HEK293 cells assessed as reduction in channel currents
Inhibition of of human TREK1 expressed in HEK293 cells assessed as reduction in channel currents
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[PMID: 26588045] |
In Vitro
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:The human gastric cancer cell line MKN45
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Concentration:10 nM
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Incubation Time:48 hours
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Result:Decreased significantly cell proliferation.
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Cell Line:The human gastric cancer cell line MKN45
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Concentration:1, 5 and 10 nM
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Incubation Time:24, 48, 72 hours
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Result:Inhibited MKN45 cell viability.
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Cell Line:The human gastric cancer cell line MKN45
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Concentration:10 nM
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Incubation Time:48 hours
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Result:Increased significantly the apoptotic cell rate.
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Cell Line:The human gastric cancer cell line MKN45
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Concentration:10 nM
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Incubation Time:48 hours
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Result:Down-regulated Cyclin D1 and up-regulated p21 expression significantly.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 137-58-6
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Appearance Solid
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Peso molecular 234.34
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Fòrmula C14H22N2O
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Color White to off-white
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SMILES
O=C(NC1=C(C)C=CC=C1C)CN(CC)CC
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Synonyms
Lignocaine
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
Publications (23)
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Journal Impact Factor
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Most Recent
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Nat Methods
2021 Jul;18(7):788-798. PMID: 34127857 -
Nat Commun
Molecular determinant of low-voltage dependence of human Nav1.7 inactivation revealed by efficacy-based Nav1.7 selective inhibitor. [Abstract]2026 Feb 10;17(1):2559. PMID: 41667447 -
Sci Adv
A worm-like nucleic acid nanostructure for gene delivery and endosomal escape via ClC3 ion exchanger. [Abstract]2026 Mar 6;12(10):eadw0891. PMID: 41790895 -
Sci Adv
EphB1-NR2B receptor signaling in glutamatergic neurons of the ventroposteromedial thalamic nucleus regulates emergence from anesthesia. [Abstract]2025 Dec 5;11(49):eadw7972. PMID: 41348875 -
J Neuroinflammation
Lidocaine alleviates morphine tolerance via AMPK-SOCS3-dependent neuroinflammation suppression in the spinal cord. [Abstract]2017 Nov 2;14(1):211. PMID: 29096659
Lidocaine purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2017 Nov 2;14(1):211. [Abstract]
Immunoblot results demonstrate that Lidocaine inhibits Morphine-induced upregulation of phosphorylation of p38 MAPK, but not the p38 total protein.
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Stem Cell Res Ther
Local anesthetics impair the growth and self-renewal of glioblastoma stem cells by inhibiting ZDHHC15-mediated GP130 palmitoylation. [Abstract]2021 Feb 4;12(1):107. PMID: 33541421
Lidocaine purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2021 Feb 4;12(1):107. [Abstract]
RT-PCR analysis of ZDHHC15 mRNA levels in GSCs treated with different concentrations (5, 10, and 20 μM) of Prilocaine, Lidocaine, Procaine, and Ropivacaine. β-Actin was used as a loading control.
Lidocaine purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2021 Feb 4;12(1):107. [Abstract]
Local anesthetics Prilocaine, Lidocaine (5-20 μM, 24-48 h), Procain, and Ropivacaine impaired cell survival through inhibition of ZDHHC15 expression.
Lidocaine purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2021 Feb 4;12(1):107. [Abstract]
Representative images showing U251 GSCs maintained under neurosphere conditions for 7 days after transfection with ZDHHC15 shRNA or treatment with prilocaine, lidocaine, procaine, or ropivacaine (20 μM).
Lidocaine purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2021 Feb 4;12(1):107. [Abstract]
Representative images showing U251 GSCs maintained under neurosphere conditions for 7 days after transfection with ZDHHC15 shRNA or treatment with prilocaine, lidocaine, procaine, or ropivacaine (20 μM). GSC neurospheres of all categories were stained for stem and differentiated cell markers as indicated. Cells were stained with antibodies against nestin and SOX2 for neural stem cell markers, and antibody staining of GFAP and MAP 2 were used as markers of differentiated cells. DAPI (4′,6-diamidino-2-phenylindole) was used as a nuclear stain.
Lidocaine purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2021 Feb 4;12(1):107. [Abstract]
The expression of GP130 in U251 GSCs (monolayer culture) transfected with ZDHHC5 shRNA and treated with Prilocaine, Lidocaine, Procaine, and Ropivacaine (20 μM) for 48 h was analyzed by immunofluorescence staining. Scale bar, 100 μm.
Lidocaine purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2021 Feb 4;12(1):107. [Abstract]
GSCs were transfected with ZDHHC5 shRNA or treated with Prilocaine, Lidocaine, Procaine, and Ropivacaine (20 μM) and harvested after 48 h. Cellular fractionation was performed to separate cytosolic and membrane fractions.
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Transl Psychiatry
Stellate ganglion block diminishes consolidation of conditioned fear memory in mice by inhibiting the locus coeruleus to the basolateral amygdala neural circuit. [Abstract]2025 May 17;15(1):172. PMID: 40382311 -
J Ethnopharmacol
Traditional Chinese Medicine YangxinDingji alleviates arrhythmias through inhibition of sodium and L-type calcium channels. [Abstract]2025 May 12:347:119803. PMID: 40239882 -
Biomater Adv
2026 Jan:178:214452. PMID: 40876091 -
Drug Des Devel Ther
Dexmedetomidine Prolongs Lidocaine Intravenous Regional Anesthesia in Rats by Blocking the Hyperpolarization-Activated Cation Current. [Abstract]2024 Apr 9:18:1103-1114. PMID: 38618283 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Int Immunopharmacol
Lidocaine inhibits influenza a virus replication by up-regulating IFNα4 via TBK1-IRF7 and JNK-AP1 signaling pathways. [Abstract]2023 Feb:115:109706. PMID: 36638664 -
Mol Med Rep
Lidocaine attenuates hypoxia/reoxygenation‑induced inflammation, apoptosis and ferroptosis in lung epithelial cells by regulating the p38 MAPK pathway. [Abstract]2022 May;25(5):150. PMID: 35244190 -
PLoS Pathog
Picornavirus infection enhances aspartate by the SLC38A8 transporter to promote viral replication. [Abstract]2023 Feb 3;19(2):e1011126. PMID: 36735752 -
Phytochemistry
Discovery of GABA-containing cyclic peptides from the cold-seep-derived fungus Aspergillus unguis SCSIO 41322 for the treatment of inflammatory bowel disease. [Abstract]2026 Aug:248:114929. PMID: 41997396 -
Reprod Toxicol
2025 May:134:108895. PMID: 40097051 -
Eur Spine J
Effect of species, concentration and volume of local anesthetics on intervertebral disk degeneration in rats with discoblock. [Abstract]2022 Nov;31(11):2960-2971. PMID: 36152221 -
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Neurogastroenterol Motil
Lidocaine ameliorates intestinal barrier dysfunction in irritable bowel syndrome by modulating corticotropin-releasing hormone receptor 2. [Abstract]2023 Nov;35(11):e14677. PMID: 37736684 -
PLoS One
The efficacy and safety of lignocaine-embedded dissolvable microneedle versus EMLA for topical analgesia in adults undergoing venepuncture: A single-centre, parallel-group, double-blind randomised clinical trial protocol in a tertiary care setting. [Abstract]2025 Nov 4;20(11):e0335932. PMID: 41187145 -
Dig Dis Sci
Lidocaine Inhibits Hepatocellular Carcinoma Development by Modulating circ_ITCH/miR-421/CPEB3 Axis. [Abstract]2021 Dec;66(12):4384-4397. PMID: 33433806 -
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Solvente y solubilidad
In Vitro:
DMSO : ≥ 100 mg/mL (426.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 5 mg/mL (21.34 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 4.35 mg/mL (18.56 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Cardiac voltage-sensitive optical mapping
Cardiac voltage-sensitive optical mapping records changes in transmembrane potential from cardiac tissue by staining the preparation with a voltage-sensitive dye and imaging fluorescence changes during electrical activation; the resulting optical action potentials can be used to map activation time, action potential duration, conduction velocity, wavefront propagation, and arrhythmia dynamics. The optical signal represents a relative fluorescence change from a tissue volume rather than a single-cell intracellular recording, so spatial resolution, sampling rate, voltage resolution, optical magnification, light penetration, and motion control must be considered together when interpreting optical action potentials.
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Cell invasion
Cell invasion is the ability of cells to migrate from one area to another via the extracellular matrix. Cell invasion is the response of normal and cancer cells to chemical and mechanical stimuli. Before migrating to a new region, the extracellular matrix is degraded by proteases within the cell. Cell invasion often occurs during wound repair, vascularization and inflammation, abnormal tissue invasion, and tumor cell metastasis.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 4.2673 mL | 21.3365 mL | 42.6730 mL | 106.6826 mL |
| 5 mM | 0.8535 mL | 4.2673 mL | 8.5346 mL | 21.3365 mL | |
| 10 mM | 0.4267 mL | 2.1337 mL | 4.2673 mL | 10.6683 mL | |
| 15 mM | 0.2845 mL | 1.4224 mL | 2.8449 mL | 7.1122 mL | |
| 20 mM | 0.2134 mL | 1.0668 mL | 2.1337 mL | 5.3341 mL | |
| DMSO | 25 mM | 0.1707 mL | 0.8535 mL | 1.7069 mL | 4.2673 mL |
| 30 mM | 0.1422 mL | 0.7112 mL | 1.4224 mL | 3.5561 mL | |
| 40 mM | 0.1067 mL | 0.5334 mL | 1.0668 mL | 2.6671 mL | |
| 50 mM | 0.0853 mL | 0.4267 mL | 0.8535 mL | 2.1337 mL | |
| 60 mM | 0.0711 mL | 0.3556 mL | 0.7112 mL | 1.7780 mL | |
| 80 mM | 0.0533 mL | 0.2667 mL | 0.5334 mL | 1.3335 mL | |
| 100 mM | 0.0427 mL | 0.2134 mL | 0.4267 mL | 1.0668 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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