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

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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.

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Metoprolol fumarate Chemical Structure

CAS No. : 80274-67-5

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Other In-stock Forms of Metoprolol fumarate:

Metoprolol succinate

Other Forms of Metoprolol fumarate:

13 Publications Citing Use of MCE Metoprolol fumarate

•Preprints. 2023 Jun 19.

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α adrenergic receptor β adrenergic receptor

Biological Activity
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References
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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.

Clinical Trial

Molecular Weight

650.80

Formula

C₃₄H₅₄N₂O₁₀

CAS No.

80274-67-5

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Ulleryd MA, et al. Metoprolol reduces proinflammatory cytokines and atherosclerosis in ApoE-/- mice. Biomed Res Int. 2014;2014:548783. [Content Brief]

[2]. Wang D, et al. Carvedilol has stronger anti-inflammation and anti-virus effects than metoprolol in murine model with coxsackievirus B3-induced viral myocarditis. Gene. 2014 Sep 1;547(2):195-201. [Content Brief]

[3]. Hajatbeigi B, et al. Cytotoxicity of Metoprolol on Leukemic Cells in Vitro. IJBC 2018; 10(4): 124-129.

[4]. Su Q, et al. Effect of metoprolol on myocardial apoptosis and caspase-9 activation after coronary microembolization in rats. Exp Clin Cardiol. 2013 Spring;18(2):161-5. [Content Brief]

Metoprolol fumarate Related Classifications

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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:

Metoprolol80274-67-5CGP 2175C Lopressor OROSAdrenergic ReceptorApoptosisBeta Receptorhypertensionischaemic heart diseaseanginaanti-inflammationanti-virusprostate cancerbreast cancerInhibitorinhibitorinhibit

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