2. Membrane Transporter/Ion Channel MAPK/ERK Pathway Stem Cell/Wnt NF-κB Apoptosis
  3. Sodium Channel MEK ERK NF-κB Apoptosis
  4. Lidocaine

リドカイン  (Synonyms: Lidocaine; Lignocaine)

製品番号: HY-B0185 純度: 99.96%
COA 取扱説明書 Technical Support

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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 137-58-6

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 60 在庫あり
Solution
10 mM * 1 mL in DMSO USD 60 在庫あり
Solid
500 mg $55 在庫あり
5 g $66 在庫あり
10 g $106 在庫あり
50 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 22 publication(s) in Google Scholar

Other Forms of Lidocaine:

リドカイン 関連抗体

Top Publications Citing Use of Products

    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.

    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.

    Sodium Channel アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8 Nav1.9

    MEK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    MEK1 MEK2 MEK5 MEK MAP2K4/MEK4 MAP2K7/MEK7

    ERK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    ERK ERK1 ERK2 ERK5 ERK8

    NF-κB アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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

     

    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]
    体外実験

    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.

    リドカイン 関連抗体

    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.
    体内実験

    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.
    臨床実験
    分子量

    234.34

    分子式

    C14H22N2O
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=C(C)C=CC=C1C)CN(CC)CC
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
    溶剤 & 溶解度
    体外: 

    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.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    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
    View the 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.

    * 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    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.

    • 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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • 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.

      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.

    • 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

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: 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)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    純度とドキュメンテーション

    純度: 99.96%

    COA (245 KB) LCMS (87 KB)

    取扱説明書 (2659 KB)
    参考文献

    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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    Lidocaine Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Lidocaine137-58-6LignocaineSodium ChannelMEKERKNF-κBApoptosisNa channelsNa+ channelsMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

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