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.

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Metoprolol Chemical Structure

Metoprolol Chemical Structure

CAS No. : 51384-51-1

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25 mg USD 90 In-stock
50 mg USD 160 In-stock
100 mg USD 300 In-stock
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Based on 13 publication(s) in Google Scholar

Other Forms of Metoprolol:

Metoprolol Related Antibodies

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  • Biological Activity

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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
=
Concentration
×
Volume
×
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 (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
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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