GLPBio

Lidocaine hydrochloride (Lignocaine hydrochloride)

Catalog No.: GC33831Purity:>98.00%
COASDSData Sheet
Lidocaine hydrochloride (Lignocaine hydrochloride) is an amino-amide-type local anaesthetic that inhibits voltage-insensitive ‘flicker’ K+ channel with an IC50 value of 220μM.

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Lidocaine hydrochloride (Lignocaine hydrochloride)
Cas No.: 73-78-9
10mM (in 1mL DMSO)In Stock
$35.00
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500mgIn Stock
$28.00
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5gIn Stock
$35.00
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10gIn Stock
$56.00
1
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Description

Lidocaine hydrochloride (Lignocaine hydrochloride) is an amino-amide-type local anaesthetic that inhibits voltage-insensitive ‘flicker’ K+ channel with an IC50 value of 220μM[1]. Lidocaine hydrochloride can cross the blood-brain barrier through passive diffusion across membranes and cause the blockade of voltage-gated sodium channels (VGSCs), leading to a reversible block of action potential propagation [2]. Lidocaine hydrochloride has been widely used in disease models for pain suppression and anti-inflammatory and anti-injury[3].

In vitro, Lidocaine hydrochloride treatment for 24h inhibited the viability of CCD-1064sk cells with an IC50 value of 613.77µM[4]. Treatment of SH-SY5Y cells with 10mM Lidocaine hydrochloride for 24h resulted in morphological changes, induced apoptosis, and significantly increased the amount of LDH released into the culture medium[5]. Treatment with 5μM Lidocaine hydrochloride for 24h attenuated cytokine-induced endothelial and vascular smooth muscle cell injury and increased cell survival[6].

In vivo, Lidocaine hydrochloride treatment (30mg/kg; twice a week) via intraperitoneal injection for 30 days reduced the tumor growth of HepG2 cell xenografts in nude mice without affecting body weight[7]. Subcutaneous injection of Lidocaine hydrochloride (30mg/kg) at 12-hour intervals for 3 days rescued the contractile function of the ischemic myocardial region in a mouse model of persistent myocardial ischemia without affecting cardiomyocyte death[8].

References:
[1] Hermanns H, Hollmann M W, Stevens M F, et al. Molecular mechanisms of action of systemic lidocaine in acute and chronic pain: a narrative review[J]. British journal of anaesthesia, 2019, 123(3): 335-349.
[2] Moreira-Junior L, Leal-Cardoso J H, Cassola A C, et al. Eugenol and lidocaine inhibit voltage-gated Na+ channels from dorsal root ganglion neurons with different mechanisms[J]. Frontiers in Pharmacology, 2024, 15: 1354737.
[3] Karnina R, Arif S K, Hatta M, et al. Molecular mechanisms of lidocaine[J]. Annals of Medicine and Surgery, 2021, 69: 102733.
[4] Choi W, Ryu H, Fuwad A, et al. Quantitative analysis of the membrane affinity of local anesthetics using a model cell membrane[J]. Membranes, 2021, 11(8): 579.
[5] Friederich P, Schmitz T P. Lidocaine-induced cell death in a human model of neuronal apoptosis[J]. European journal of anaesthesiology, 2002, 19(8): 564-570.
[6] de Klaver M J M, Buckingham M G, Rich G F. Lidocaine attenuates cytokine-induced cell injury in endothelial and vascular smooth muscle cells[J]. Anesthesia & Analgesia, 2003, 97(2): 465-470.
[7] Xing W, Chen D T, Pan J H, et al. Lidocaine induces apoptosis and suppresses tumor growth in human hepatocellular carcinoma cells in vitro and in a xenograft model in vivo[J]. Anesthesiology, 2017, 126(5): 868-881.
[8] Müller-Edenborn B, Kania G, Osto E, et al. Lidocaine enhances contractile function of ischemic myocardial regions in mouse model of sustained myocardial ischemia[J]. PloS one, 2016, 11(5): e0154699.

Protocol

Cell experiment [1]:

Cell lines

MDA-MB-231 cells

Preparation Method

MDA-MB-231 cells were cultured in Dulbecco's modified Eagle's medium (DMEM) containing 4.5g/L D-glucose and glutaMAX supplemented with 10% fetal bovine serum and 1% penicillin-streptomycin. Cells were incubated under standard culture conditions (CO2 5%, O2 95%, 37°C), and experiments were performed at 70% to 100% confluency. MDA-MB-231 cells were cultured in six-well plates and incubated for 24 hours with Lidocaine hydrochloride (100μM). A scratch was created in each well using a small pipettor tip, and the migration of cells was stimulated with 0.1μM CXCL12, after which the scratch wound area was quantified.

Reaction Conditions

100μM; 24h

Applications

Lidocaine hydrochloride treatment significantly inhibited CXCL12-induced in vitro migration of MDA-MB-231 cells.
Animal experiment [2]:

Animal models

BALB/c nude mice

Preparation Method

HepG2 cells (2×106) were subcutaneously injected into the right axilla of BALB/c nude mice. The mice were randomly divided into a control group, Lidocaine hydrochloride group, and cisplatin group (n=8 in each group). When the palpable tumor volume reached approximately 50mm3, mice were intraperitoneally injected with PBS solution (as a control), Lidocaine hydrochloride (30mg/kg; twice a week), and cisplatin (3mg/kg; once a week), and tumor growth was observed for 30 days. Tumor width and length were measured every 3 days. Tumor volume was calculated as (length × width2)/2. The body weight of mice was also recorded.

Dosage form

3mg/kg; twice a week for 30 days; i.p.

Applications

Lidocaine hydrochloride treatment inhibited the tumor growth of HepG2 cell xenografts in nude mice without affecting body weight.

References:
[1] D'agostino G, Saporito A, Cecchinato V, et al. Lidocaine inhibits cytoskeletal remodelling and human breast cancer cell migration[J]. British journal of anaesthesia, 2018, 121(4): 962-968.
[2] Xing W, Chen D T, Pan J H, et al. Lidocaine induces apoptosis and suppresses tumor growth in human hepatocellular carcinoma cells in vitro and in a xenograft model in vivo[J]. Anesthesiology, 2017, 126(5): 868-881.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
73-78-9
SMILES
O=C(NC1=C(C)C=CC=C1C)CN(CC)CC.[H]Cl
Molecular Formula
C14H23ClN2O
Molecular Weight
270.8
Solubility
Water : ≥ 36 mg/mL (132.94 mM)
Storage
4°C, protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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