Art. -Nr.: HY-B0185

Lidocaine

(Synonyms: Lignocaine)

22 Cited Publications

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Based on 22 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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Reinheit: 99.96%
CAS. Nr.: 137-58-6
Formel: C₁₄H₂₂N₂O
Molecular Weight:234.34

Speicherung:

4°C, protect from light

* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Lidocaine Chemical Structure

CAS. Nr.: 137-58-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (22)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

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 an amide derivative and has potential for the research of ventricular arrhythmia^[2].

IC₅₀ & Target^[1,2]

MEK

ERK

NF-κB

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Alle MEK Isoform-spezifische Produkte anzeigen :

Alle ERK Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>500 μM Compound: lidocaine	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	[PMID: 23241029]
HEK293	IC₅₀	180 μM Compound: 1	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	[PMID: 23121096]
HEK293	IC₅₀	207 μM Compound: 35	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	[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.

Cell Proliferation Assay^[2]

Cell Line:

The human gastric cancer cell line MKN45
Concentration:

10 nM
Incubation Time:

48 hours
Result:

Decreased significantly cell proliferation.

Cell Viability Assay^[2]

Cell Line:

The human gastric cancer cell line MKN45
Concentration:

1, 5 and 10 nM
Incubation Time:

24, 48, 72 hours
Result:

Inhibited MKN45 cell viability.

Apoptosis Analysis^[2]

Cell Line:

The human gastric cancer cell line MKN45
Concentration:

10 nM
Incubation Time:

48 hours
Result:

Increased significantly the apoptotic cell rate.

Western Blot Analysis^[2]

Cell Line:

The human gastric cancer cell line MKN45
Concentration:

10 nM
Incubation Time:

48 hours
Result:

Down-regulated Cyclin D1 and up-regulated p21 expression significantly.

In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 137-58-6
Appearance Solid
Molecular Weight 234.34
Formel C₁₄H₂₂N₂O
Color White to off-white
SMILES

O=C(NC1=C(C)C=CC=C1C)CN(CC)CC
Synonyms

Lignocaine
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Publications (22)

All RT-PCRCell Proliferation/Viability AssayCell Imaging/StainingWB

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Journal Impact Factor

Nat Methods

Metabolomic profiling of single enlarged lysosomes. [Abstract]

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.
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.
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
Biomater Adv

Hydrogel-based drug delivery system designed for chemotherapy-induced alopecia. [Abstract]

2025 Aug 15:178:214452. PMID: 40876091
J Ethnopharmacol

Traditional Chinese Medicine YangxinDingji alleviates arrhythmias through inhibition of sodium and L-type calcium channels. [Abstract]

2025 Apr 14:347:119803. PMID: 40239882
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
PLoS Pathog

Picornavirus infection enhances aspartate by the SLC38A8 transporter to promote viral replication. [Abstract]

2023 Feb 3;19(2):e1011126. PMID: 36735752
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
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
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
J Phys D Appl Phys

2019 Aug; 52(46).
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
Reprod Toxicol

Zebrafish embryos as a teratogenicity screening tool to reduce potential birth defects. [Abstract]

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
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
Eng Proc

2026 Jan 14;110(1):7.
University of Glasgow

2023.

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.2673 mL

21.3365 mL

42.6730 mL

5 mM

0.8535 mL

4.2673 mL

8.5346 mL

10 mM

0.4267 mL

2.1337 mL

4.2673 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (10.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
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- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

Lidocaine

22 Cited Publications

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Lidocaine

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Publications Citing Use of MedChemExpress (MCE) Lidocaine

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Alle MEK Isoform-spezifische Produkte anzeigen