1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel
  3. Amlodipine

Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer.

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

CAS No. : 88150-42-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Amlodipine:

Top Publications Citing Use of Products

    Amlodipine purchased from MedChemExpress. Usage Cited in: Food Chem Toxicol. 2025 Feb 10:115317.  [Abstract]

    A CCK-8 assay was used to detect the effect of AMs on the proliferation of Ishikawa cells. The results showed that the half-maximal inhibitory concentration (IC50) of Amlodipine (AM) against Ishikawa cells (at 72 h) was 12.36 μM.

    Amlodipine purchased from MedChemExpress. Usage Cited in: Food Chem Toxicol. 2025 Feb 10:115317.  [Abstract]

    Cell apoptosis rate was detected by flow cytometry using Annexin-V/PI staining. The results showed that the apoptotic rate of the Amlodipine (AM) (15 μM; 12 h)-treated Ishikawa cells was 16.8%, which was 2.16-fold higher than that in cells treated with DMSO.

    Amlodipine purchased from MedChemExpress. Usage Cited in: Food Chem Toxicol. 2025 Feb 10:115317.  [Abstract]

    EdU staining showing the effect of Amlodipine (AM) (15 μM; 48 h) on Ishikawa cells. The EdU staining assay revealed that the EdU-positive rate of the AM-treated Ishikawa cells was significantly reduced compared with that of the control group.

    Amlodipine purchased from MedChemExpress. Usage Cited in: Food Chem Toxicol. 2025 Feb 10:115317.  [Abstract]

    Amlodipine (AM) (15 or 20 mg/kg; i.p.; every other day for two weeks) inhibited tumor growth in a dose-dependent manner in BALB/c nude mice bearing subcutaneous xenografts established from Ishikawa cells.

    Amlodipine purchased from MedChemExpress. Usage Cited in: Food Chem Toxicol. 2025 Feb 10:115317.  [Abstract]

    H&E and PCNA staining of sections from mice treated with Amlodipine (AM) (15 or 20 mg/kg; i.p.; every other day for two weeks).

    Amlodipine purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2021 Apr;53(4):572-590.  [Abstract]

    Rat GMCs pretreated with the calcium channel blocker Amlodipine (10μM), inhibitors of PKC (Go6983; 10μM), c-Raf (AZ628, 10μM) and MEK1/2 (U0126, 10μM) for 30min were stimulated with sublytic C5b-9 for 4 0min or 2h. The intracellular calcium was determined by Fluo-4 AM. The results showed that Amlodipine effectively blocked the rise in intracellular calcium levels in rat GMCs induced by 40 min of sublytic C5b-9 stimulation.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer[1][2][3].

    IC50 & Target[1]

    L-type calcium channel

     

    Cellular Effect
    Cell Line Type Value Description References
    LLC-MK2 IC50
    70.82 μM
    Compound: Amlodipine
    Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
    Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
    [PMID: 20934347]
    LLC-MK2 IC50
    8.07 μM
    Compound: Amlodipine
    Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
    Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
    [PMID: 20934347]
    LLC-PK1 IC50
    22 μM
    Compound: Amlodipine
    TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells
    TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells
    [PMID: 11145223]
    Oocyte IC50
    1.2 μM
    Compound: Amlodipine
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
    [PMID: 22761000]
    Oocyte IC50
    4.2 μM
    Compound: Amlodipine
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
    [PMID: 22761000]
    Ventricular myocyte IC50
    0.57 μM
    Compound: Amlodipine
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    [PMID: 22761000]
    In Vitro

    Amlodipine (20-40 μM; 48 h) reduces BrdU incorporation to 68.6% and 26.3% at concentrations of 20 and 30 μM in A431 cells, respectively[3].
    Amlodipine (30 μM; pretreated for 1 h) significantly attenuates the uridine 5′-triphosphate (UTP)-induced increases of [Ca2+]i in A431 cells[3].
    Amlodipine (30 μM) inhibits the store-operated Ca2+influx evoked by Thapsigargin in Fluo-3-loaded cells[3].

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

    In Vivo

    Amlodipine (5 mg/kg/day; s.c. for 2 weeks) significantly decreases systolic blood pressure (SBP) in VSMC ATP2B1 KO mice[4].
    Amlodipine (10 mg/kg; i.p. once daily for 20 days) causes a significant retardation of tumor growth and prolongs the survival of A431 tumor-bearing mice[3].

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

    Animal Model: ATP2B1loxP/loxP mice[4]
    Dosage: 5 mg/kg/day
    Administration: Subcutaneously implanted osmotic pump for 2 weeks
    Result: Significantly decreased the blood pressure.
    Molecular Weight

    408.88

    Formula

    C20H25ClN2O5

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(OCC)C1=C(NC(C)=C(C1C2=CC=CC=C2Cl)C(OC)=O)COCCN

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 31.25 mg/mL (76.43 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 2.4457 mL 12.2285 mL 24.4571 mL
    5 mM 0.4891 mL 2.4457 mL 4.8914 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. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • 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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    Volume (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: ≥ 3 mg/mL (7.34 mM); Clear solution

      This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: 3 mg/mL (7.34 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 3 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
    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).
    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: 99.87%

    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, 1 year; -20°C, 6 months. 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
    DMSO 1 mM 2.4457 mL 12.2285 mL 24.4571 mL 61.1426 mL
    5 mM 0.4891 mL 2.4457 mL 4.8914 mL 12.2285 mL
    10 mM 0.2446 mL 1.2229 mL 2.4457 mL 6.1143 mL
    15 mM 0.1630 mL 0.8152 mL 1.6305 mL 4.0762 mL
    20 mM 0.1223 mL 0.6114 mL 1.2229 mL 3.0571 mL
    25 mM 0.0978 mL 0.4891 mL 0.9783 mL 2.4457 mL
    30 mM 0.0815 mL 0.4076 mL 0.8152 mL 2.0381 mL
    40 mM 0.0611 mL 0.3057 mL 0.6114 mL 1.5286 mL
    50 mM 0.0489 mL 0.2446 mL 0.4891 mL 1.2229 mL
    60 mM 0.0408 mL 0.2038 mL 0.4076 mL 1.0190 mL
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