2. GPCR/G Protein Neuronal Signaling Apoptosis
  3. Adrenergic Receptor Apoptosis
  4. Metoprolol

Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties.

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

CAS No. : 51384-51-1

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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 15 publication(s) in Google Scholar

Other Forms of Metoprolol:

Metoprolol Related Antibodies

Top Publications Citing Use of Products

    Metoprolol purchased from MedChemExpress. Usage Cited in: J Intern Med. 2024 Sep;296(3):291-297.  [Abstract]

    Selective blockers Metoprolol (METO; β1-AR blocker; 10 µmol/L) and ICI118551 (ICI; β2-AR blocker; 10 µmol/L) were used to explore the interactions of the spike protein with β1-AR and β2-AR, respectively.

    Metoprolol purchased from MedChemExpress. Usage Cited in: J Intern Med. 2024 Sep;296(3):291-297.  [Abstract]

    cAMP accumulation in NMCMs treated with ISO (1 µmol/L) and the spike trimer (10 nmol/L) with or without pretreatment with Metoprolol (10 µmol/L) and ICI118551 (10 µmol/L).

    Metoprolol purchased from MedChemExpress. Usage Cited in: SSRN. 2024 May 30.

    Quantification of immunofluorescence staining of phosphorylated-GSK3β in NRCFs. The ratio of phosphorylated protein to total protein reflects the activation of signaling pathways. NRCFs were starved for 24h. Mig and Metoprolol (Met: 10 μM) were added ahead for 1h, then ISO was added for 24h. Met was used as positive control.

    View All Adrenergic Receptor Isoform Specific Products:

    View All Isoforms
    α adrenergic receptor β adrenergic receptor

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3].

    IC50 & Target

    β1 adrenoceptor

     

    Cellular Effect
    Cell Line Type Value Description References
    A-375 IC50
    > 100 μM
    Compound: Metoprolol
    Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    		[PMID: 32216987]
    HEK293 IC50
    > 1000 μM
    Compound: 95
    Inhibition of RyR2 R4496C mutant (unknown origin)-mediated store-overload induced calcium release expressed in HEK293 cells after 8 to 10 mins by fura-2/AM dye-based fluorescence assay
    Inhibition of RyR2 R4496C mutant (unknown origin)-mediated store-overload induced calcium release expressed in HEK293 cells after 8 to 10 mins by fura-2/AM dye-based fluorescence assay
    		[PMID: 24124794]
    SK-MEL-28 IC50
    > 100 μM
    Compound: Metoprolol
    Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    		[PMID: 32216987]
    SK-MEL-5 IC50
    > 100 μM
    Compound: Metoprolol
    Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    		[PMID: 32216987]
    In Vitro

    Metoprolol (0-1000 μg/mL; 24-72 h) shows cytotoxic effect on U937 and MOLT-4 cells dose and time dependently[3].

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

    Metoprolol Related Antibodies

    Cell Cytotoxicity Assay[3]

    Cell Line: U937 and MOLT-4 cells
    Concentration: 1, 10, 50, 100, 500 and 1000 μg/mL
    Incubation Time: 24, 48 and 72 h
    Result: Significantly decreased the viability of U937 and MOLT-4 cells at 1000 μg/mL (3740.14µM) concentration after 48 hours incubation time, significantly reduced the viability of U937 cells at ≥500 μg/ml (≥1870.07µM) concentrations after 72 hours incubation time, and significantly decreased the viability of MOLT4 cells at ≥100 μg/ml (≥374.01µM) concentrations after 72 hours incubation.
    In Vivo

    Metoprolol (2.5 mg/kg/h; infusion; 11 weeks) reduces proinflammatory cytokines and atherosclerosis in ApoE?/? Mice[1].
    Metoprolol (15 mg/kg/q12h; i.g.; 5 days) shows anti-inflammation and anti-virus effects in murine model with coxsackievirus B3-induced viral myocarditis[2].
    Metoprolol (2.5 mg/kg; i.v.; 3 bolus injections) significantly decreased activated caspase-9 protein expression and inhibits myocardial apoptosis in coronary microembolization (CME) rats[4].

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

    Animal Model: Male ApoE−/− mice[1]
    Dosage: 2.5 mg/kg/h
    Administration: Via osmotic minipumps, 11 weeks
    Result: Significantly reduced atherosclerotic plaque area in thoracic aorta, reduced serum TNFα and the chemokine CXCL1 as well as decreasing the macrophage content in the plaques.
    Animal Model: Balb/c mice, coxsackievirus B3 (CVB3) induced viral myocarditis (VMC) model[2]
    Dosage: 15 mg/kg/q12h
    Administration: Oral gavage, 5 consecutive days
    Result: Reduced pathological scores of VMC induced by CVB3 infection, protected the myocardium against viral damage by reducing serum cTn-I levels. Decreased the levels of myocardial pro-inflammatory cytokines and increase the expression of anti-inflammatory cytokine. Significantly decreased myocardial virus titers.
    Clinical Trial
    Molecular Weight

    267.36

    Formula

    C15H25NO3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC(CNC(C)C)COC1=CC=C(CCOC)C=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (374.03 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 3.7403 mL 18.7014 mL 37.4028 mL
    5 mM 0.7481 mL 3.7403 mL 7.4806 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 (protect from light). 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    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 (9.35 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 (9.35 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.
    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 (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.
    Purity & Documentation

    Purity: 99.99%

    SDS (394 KB)

    COA (242 KB) HNMR (161 KB) RP-HPLC (254 KB) MS (68 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 (protect from light). 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 3.7403 mL 18.7014 mL 37.4028 mL 93.5069 mL
    5 mM 0.7481 mL 3.7403 mL 7.4806 mL 18.7014 mL
    10 mM 0.3740 mL 1.8701 mL 3.7403 mL 9.3507 mL
    15 mM 0.2494 mL 1.2468 mL 2.4935 mL 6.2338 mL
    20 mM 0.1870 mL 0.9351 mL 1.8701 mL 4.6753 mL
    25 mM 0.1496 mL 0.7481 mL 1.4961 mL 3.7403 mL
    30 mM 0.1247 mL 0.6234 mL 1.2468 mL 3.1169 mL
    40 mM 0.0935 mL 0.4675 mL 0.9351 mL 2.3377 mL
    50 mM 0.0748 mL 0.3740 mL 0.7481 mL 1.8701 mL
    60 mM 0.0623 mL 0.3117 mL 0.6234 mL 1.5584 mL
    80 mM 0.0468 mL 0.2338 mL 0.4675 mL 1.1688 mL
    100 mM 0.0374 mL 0.1870 mL 0.3740 mL 0.9351 mL
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    Metoprolol 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:

    Metoprolol51384-51-1Adrenergic ReceptorApoptosisBeta Receptorhypertensionischaemic heart diseaseanginaanti-inflammationanti-virusprostate cancerbreast cancerInhibitorinhibitorinhibit

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