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  3. Metoprolol fumarate

Metoprolol fumarate  (Synonyms: CGP 2175C; Lopressor OROS)

Cat. No.: HY-17503C
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Metoprolol fumarate (CGP 2175C) is an orally active, selective β1-adrenoceptor antagonist. Metoprolol fumarate shows anti-inflammation, antitumor and anti-angiogenic properties.

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

CAS No. : 80274-67-5

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Top Publications Citing Use of Products

    Metoprolol fumarate 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 fumarate 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 fumarate 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.

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    Description

    Metoprolol fumarate (CGP 2175C) is an orally active, selective β1-adrenoceptor antagonist. Metoprolol fumarate shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3].

    IC50 & Target

    β1 adrenoceptor

     

    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.

    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.
    Molecular Weight

    650.80

    Formula

    C34H54N2O10

    CAS No.
    SMILES

    OC(CNC(C)C)COC1=CC=C(CCOC)C=C1.O=C(O)/C=C/C(O)=O.OC(CNC(C)C)COC2=CC=C(CCOC)C=C2

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    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

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    • 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.

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    Product Name:
    Metoprolol fumarate
    Cat. No.:
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