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

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

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

Flunarizine dihydrochloride Chemical Structure

Flunarizine dihydrochloride Chemical Structure

CAS No. : 30484-77-6

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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 dihydrochloride:

Top Publications Citing Use of Products

    Flunarizine dihydrochloride 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.

    Flunarizine dihydrochloride 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 dihydrochloride 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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target[1][3]

    T-type calcium channel

     

    D2 Receptor

     

    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.

    Cell Viability Assay[4]

    Cell Line: Chromaffin cells
    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

    477.42

    Formula

    C26H28Cl2F2N2

    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.Cl.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (104.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 1 mg/mL (2.09 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0946 mL 10.4730 mL 20.9459 mL
    5 mM 0.4189 mL 2.0946 mL 4.1892 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * 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
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 (5.24 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 (5.24 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: 10 mg/mL (20.95 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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
    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 (sealed storage, away from moisture). 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
    H2O / DMSO 1 mM 2.0946 mL 10.4730 mL 20.9459 mL 52.3648 mL
    DMSO 5 mM 0.4189 mL 2.0946 mL 4.1892 mL 10.4730 mL
    10 mM 0.2095 mL 1.0473 mL 2.0946 mL 5.2365 mL
    15 mM 0.1396 mL 0.6982 mL 1.3964 mL 3.4910 mL
    20 mM 0.1047 mL 0.5236 mL 1.0473 mL 2.6182 mL
    25 mM 0.0838 mL 0.4189 mL 0.8378 mL 2.0946 mL
    30 mM 0.0698 mL 0.3491 mL 0.6982 mL 1.7455 mL
    40 mM 0.0524 mL 0.2618 mL 0.5236 mL 1.3091 mL
    50 mM 0.0419 mL 0.2095 mL 0.4189 mL 1.0473 mL
    60 mM 0.0349 mL 0.1745 mL 0.3491 mL 0.8727 mL
    80 mM 0.0262 mL 0.1309 mL 0.2618 mL 0.6546 mL
    100 mM 0.0209 mL 0.1047 mL 0.2095 mL 0.5236 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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      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.

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    Product Name:
    Flunarizine dihydrochloride
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