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Metoprolol Tartrate Adrenergic Receptor antagonist

Cat.No.S1856

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

Chemical Structure

Molecular Weight: 684.81

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 684.81 Formula

2C15H25NO3.C4H6O6

Storage (From the date of receipt)
CAS No. 56392-17-7 Download SDF Storage of Stock Solutions

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (146.02 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
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]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06004453 Recruiting
Heart Failure
Novartis Pharmaceuticals|Novartis
April 4 2023 --
NCT05368831 Completed
Healthy Volunteers
NorthSea Therapeutics B.V.
July 19 2022 Phase 1
NCT05171985 Unknown status
COVID-19 Pneumonia|Atrial Fibrillation
Tanta University
January 2022 Not Applicable
NCT04842981 Terminated
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

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