2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. Calcium Channel Sodium Channel Dopamine Receptor
  4. Flunarizine

Flunarizine is a potent dual Na+/Ca2+ channel (T-type) blocker. Flunarizine is a D2 dopamine receptor antagonist. Flunarizine shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects.

For research use only. We do not sell to patients.

Flunarizine Chemical Structure

Flunarizine Chemical Structure

CAS No. : 52468-60-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Flunarizine:

Flunarizine Related Antibodies

Top Publications Citing Use of Products

    Flunarizine purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Nov 16;8(1):16932.   [Abstract]

    Western blot analysis of SUM149PT cells treated by FLN (20 μM, 48 h).

    Flunarizine purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Nov 16;8(1):16932.   [Abstract]

    FLN enhances autophagic influx and N-Ras translocation to autophagosomes. Cells co-transfected with mCherry-N-Ras and EGFP-LC3 are imaged by confocal microscopy after FLN treatment.

    Flunarizine purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Nov 16;8(1):16932.   [Abstract]

    SUM149PT cells are first treated with FLN as in panel-A, followed by autophagy inhibitors 3-MA (5 mM), chloroquine (20 μM) or bafilomycin A1 (20 nM) for another 24 hours. The proteasome inhibitor MG132 (15 μM) is included as a negative control to show unabated N-Ras reduction. The cells are then harvested and analyzed by Western blot.

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    Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Flunarizine is a potent dual Na+/Ca2+ channel (T-type) blocker. Flunarizine is a D2 dopamine receptor antagonist. Flunarizine shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects[1][2][3][4][5].

    IC50 & Target[1][2]

    D2 Receptor

     

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    0.08 μM
    Compound: Flunarizine
    Blocking of rat N-type calcium channel alpha-1B/alpha-2-delta-1/beta-1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
    Blocking of rat N-type calcium channel alpha-1B/alpha-2-delta-1/beta-1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
    		[PMID: 19815411]
    HEK293 IC50
    0.31 μM
    Compound: Flunarizine
    Blocking of rat Voltage-dependent L-type calcium channel alpha1c/alpha2delta-1/beta1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
    Blocking of rat Voltage-dependent L-type calcium channel alpha1c/alpha2delta-1/beta1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
    		[PMID: 19815411]
    In Vitro

    Flunarizine blocks sodium currents (INa) and calcium currents (ICa) with IC50 values of 0.94 μM and 1.77 μM in cultured rat cortical neurons, respectively[2].
    Flunarizine (10 and 30 μM; 24 h) shows cytotoxic effects to chromaffin cells[4].
    Flunarizine (1-30 μM) causes clear cytoprotection of chromaffin cell at concentrations of 3-10 μM[4].

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

    Flunarizine Related Antibodies

    Cell Cytotoxicity Assay[4]

    Cell Line: Chromaffin cells[4]
    Concentration: 10 and 30 μM
    Incubation Time: 24 hours
    Result: Showed a tendency to increase cell death at the concentration of 10 μM, and showed near 100% cell loss at the concentration of 30 μM.
    In Vivo

    Flunarizine (intraperitoneal injection; 30?mg/kg; once) protects mice from lipopolysaccharide- (LPS-) induced acute lung injury (ALI)[5].

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

    Animal Model: Male BALB/c mice (6-8 weeks old) with acute lung injury induced by lipopolysaccharide[5]
    Dosage: 30 mg/kg
    Administration: Intraperitoneal injection; 30 mg/kg; once
    Result: Suppressed the LPS-induced cell influx, protein leakage, and inflammatory cytokines release.
    Inhibited the pulmonary inflammation.
    Clinical Trial
    Molecular Weight

    404.49

    Formula

    C26H26F2N2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    FC1=CC=C(C(N2CCN(C/C=C/C3=CC=CC=C3)CC2)C4=CC=C(F)C=C4)C=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (247.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4722 mL 12.3612 mL 24.7225 mL
    5 mM 0.4944 mL 2.4722 mL 4.9445 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.18 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.18 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.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    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).
    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.
    Purity & Documentation

    Purity: 99.93%

    SDS (251 KB)

    COA (246 KB) HNMR (275 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4722 mL 12.3612 mL 24.7225 mL 61.8062 mL
    5 mM 0.4944 mL 2.4722 mL 4.9445 mL 12.3612 mL
    10 mM 0.2472 mL 1.2361 mL 2.4722 mL 6.1806 mL
    15 mM 0.1648 mL 0.8241 mL 1.6482 mL 4.1204 mL
    20 mM 0.1236 mL 0.6181 mL 1.2361 mL 3.0903 mL
    25 mM 0.0989 mL 0.4944 mL 0.9889 mL 2.4722 mL
    30 mM 0.0824 mL 0.4120 mL 0.8241 mL 2.0602 mL
    40 mM 0.0618 mL 0.3090 mL 0.6181 mL 1.5452 mL
    50 mM 0.0494 mL 0.2472 mL 0.4944 mL 1.2361 mL
    60 mM 0.0412 mL 0.2060 mL 0.4120 mL 1.0301 mL
    80 mM 0.0309 mL 0.1545 mL 0.3090 mL 0.7726 mL
    100 mM 0.0247 mL 0.1236 mL 0.2472 mL 0.6181 mL
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    Flunarizine Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      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:

    Flunarizine52468-60-7Calcium ChannelSodium ChannelDopamine ReceptorCa2+ channelsCa channelsNa channelsNa+ channelsanticonvulsive activityantimigraine activityperipheral vasodilator effectchromaffin cellcultured rat cortical neuronsInhibitorinhibitorinhibit

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