Metoprolol fumarate
Based on 15 publication(s) in Google Scholar
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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- CAS No.: 80274-67-5
- Formule: C34H54N2O10
- Masse moléculaire:650.80
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Activité biologique
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Metoprolol fumarate
More- Phytomedicine. 2026 Oct:160:158619.
- Mol Med. 2025 Feb 11;31(1):55.
- Emerg Contam. 2026 Feb 23.
- J Intern Med. 2024 Sep;296(3):291-297. [Abstract]
- Eur J Med Chem. 2024 Dec 5:279:116842. [Abstract]
- Int J Mol Sci. 2026 Apr 15;27(8):3523. [Abstract]
- Int Immunopharmacol. 2024 Oct 25:140:112894. [Abstract]
- iScience. 2025 Jan 17;28(2):111831. [Abstract]
- J Pharm Biomed Anal. 2021 Feb 20:195:113870. [Abstract]
- J Pharmacol Sci. 2020 Sep;144(1):30-42. [Abstract]
- Biochem Biophys Res Commun. 2025 Oct 30:786:152756. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2023 Jul 1:1227:123804. [Abstract]
- Environ Toxicol. 2024 Mar;39(3):1682-1699. [Abstract]
- Preprints. 2023 Jun 19.
- Chemosphere. 2019 Jun:225:378-387. [Abstract]
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Activité biologique
Description
IC50 & Target
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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. Further protocols information, click here.
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Cell Line:U937 and MOLT-4 cells
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Concentration:1, 10, 50, 100, 500 and 1000 μg/mL
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Incubation Time:24, 48 and 72 h
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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 (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.
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Animal Model:Male ApoE−/− mice[1]
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Dosage:2.5 mg/kg/h
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Administration:Via osmotic minipumps, 11 weeks
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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.
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Animal Model:Balb/c mice, coxsackievirus B3 (CVB3) induced viral myocarditis (VMC) model[2]
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Dosage:15 mg/kg/q12h
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Administration:Oral gavage, 5 consecutive days
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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.
Chemical Information
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CAS No. 80274-67-5
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Masse moléculaire 650.80
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Formule C34H54N2O10
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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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Synonyms
CGP 2175C; Lopressor OROS
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (15)
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Journal Impact Factor
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Most Recent
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Metoprolol fumarate purchased from MedChemExpress. Usage Cited in: Mol Med. 2025 Feb 11;31(1):55.
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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J Intern Med
SARS-CoV-2 spike protein acts as a β-adrenergic receptor agonist: A potential mechanism for cardiac sequelae of long COVID. [Abstract]2024 Sep;296(3):291-297. PMID: 39073192
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).
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Eur J Med Chem
2024 Dec 5:279:116842. PMID: 39260319 -
Int J Mol Sci
N- p- trans-Coumaroyltyramine Improves Myocardial Ischemia-Reperfusion Injury: From Cellular Protection to Animal Model Validation and the Discovery of the Target Tcap. [Abstract]2026 Apr 15;27(8):3523. PMID: 42074166 -
Int Immunopharmacol
Baricitinib alleviates cardiac fibrosis and inflammation induced by chronic sympathetic activation. [Abstract]2024 Oct 25:140:112894. PMID: 39126736 -
iScience
Stimulation of TRPV1+ peripheral somatosensory nerves suppress inflammation via the somato-autonomic reflex. [Abstract]2025 Jan 17;28(2):111831. PMID: 39967868 -
J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569 -
J Pharmacol Sci
Sustained increased CaMKII phosphorylation is involved in the impaired regression of isoproterenol-induced cardiac hypertrophy in rats. [Abstract]2020 Sep;144(1):30-42. PMID: 32665128 -
Biochem Biophys Res Commun
Dual-cardiotoxicity evaluation of torsadogenic risk drugs using human iPSC-derived cardiomyocytes. [Abstract]2025 Oct 30:786:152756. PMID: 41043280 -
J Chromatogr B Analyt Technol Biomed Life Sci
High-throughput screening of LogD by using a sample pooling approach based on the traditional shake flask method. [Abstract]2023 Jul 1:1227:123804. PMID: 37393793 -
Environ Toxicol
Phenylacetyl glutamine (PAGln) enhances cardiomyocyte death after myocardial infarction through β1 adrenergic receptor. [Abstract]2024 Mar;39(3):1682-1699. PMID: 38041472 -
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Chemosphere
Mass-balance-model-based evaluation of sewage treatment plant contribution to residual pharmaceuticals in environmental waters. [Abstract]2019 Jun:225:378-387. PMID: 30884299
Protocole
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureté et documentation
Références
[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]
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Metoprolol fumarate Related Classifications
HY-17503C Related Classifications
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