Metoprolol Tartrate

For research use only.

Catalog No.S1856 Synonyms: CGP 2175E

Metoprolol Tartrate Chemical Structure

CAS No. 56392-17-7

Metoprolol Tartrate (CGP 2175E) is a selective β1 receptor blocker medication, used to treat hypertension and heart failure.

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Biological Activity

Description Metoprolol Tartrate (CGP 2175E) is a selective β1 receptor blocker medication, used to treat hypertension and heart failure.
Targets
β-adrenergic receptor [1]
In vitro

Metoprolol, attenuates cardiomyocyte apoptosis in left ventricular (LV) myocardium of dogs with heart failure (HF). Metoprolol induces the expression of Bcl-2 independent of heart failure (HF) and that this independently confers protection. [1]

In vivo Metoprolol partly reverses the depressed left ventricular (LV) systolic pressure, positive and negative rates of changes in pressure development, ejection fraction, fractional shortening and cardiac output, as well as increased LV end-diastolic pressure in 20 weeks myocardial infarction (MI) rats. Metoprolol partially reverses the elevated levels of plasma norepinephrine and dopamine without affecting the elevated levels of epinephrine. [2] Metoprolol treatment attenuates the development of cardiac dysfunction in streptozotocin (STZ)-diabetic rats. Metoprolol leads to reduced rates of palmitate oxidation, stimulation of glucose oxidation, and increases tissue ATP levels. Metoprolol leads to decreased maximum activity and decreased sensitivity of carnitine palmitoyltransferase I to malonyl-CoA. Metoprolol also increases sarco(endo) plasmic reticulum Ca(2+)-ATPase expression and prevents the reexpression of atrial natriuretic peptide in diabetic hearts of in streptozotocin (STZ)-diabetic rats. [3] Metoprolol, attenuates the increase in collagen content in noninfarcted regions and prevents the increase in right ventricular weight/body weight, and its effect is similar to captopril in rat model with myocardial infarction (MI). Metoprolol treatment tends to increase right ventricular weight and heart weight. [4]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (146.02 mM)
Water 100 mg/mL (146.02 mM)
Ethanol 31 mg/mL (45.26 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 684.81
Formula

2C15H25NO3.C4H6O6

CAS No. 56392-17-7
Storage powder
in solvent
Synonyms CGP 2175E
Smiles CC(C)NCC(COC1=CC=C(C=C1)CCOC)O.CC(C)NCC(COC1=CC=C(C=C1)CCOC)O.C(C(C(=O)O)O)(C(=O)O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04842981 Recruiting Drug: Tocilizumab|Drug: Sarilumab Arthritis Rheumatoid|Interaction University of Southern Denmark|Odense University Hospital|Hospital of South West Jutland|King Christian X´Hospital for Rheumatic Diseases|Sygehus Lillebaelt|Odense Patient Data Explorative Network May 25 2021 Phase 1|Phase 2
NCT04840641 Recruiting Drug: Flucloxacillin Healthy Volunteers|Drug Drug Interaction University of Southern Denmark|SignaTope GmbH Germany March 25 2021 Phase 1
NCT03082352 Unknown status Drug: BF-Metoprolol Tablet 100mg|Drug: Betaloc Tablet 100mg Healthy Bright Future Pharmaceuticals Factory O/B Bright Future Pharmaceutical Laboratories Limited|Chinese University of Hong Kong August 2020 Phase 1

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Adrenergic Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID