Home Endocrinology & Hormones Mineralocorticoid Receptor antagonist Eplerenone For research use only.

Eplerenone

Synonyms: CGP 30083, SC-66110

Eplerenone is a mineralocorticoid receptor antagonist, and blocks the action of aldosterone, used to control high blood pressure.

Eplerenone Chemical Structure

Eplerenone Chemical Structure

CAS No. 107724-20-9

Purity & Quality Control

Eplerenone Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Huh7 cells Function assay Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay, IC50=0.122 μM 20672822
COS1 cells Function assay 1 days Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay, IC50=1.3 μM 22074142
293 cells Function assay 16 h Displacement of [3H]aldosterone from human mineralocorticoid receptor expressed in 293 cells after 16 hrs by scintillation counting, IC50=2.6 μM 25187277
Click to View More Cell Line Experimental Data

Biological Activity

Description Eplerenone is a mineralocorticoid receptor antagonist, and blocks the action of aldosterone, used to control high blood pressure.
Targets
mineralocorticoid receptor [1]
In Vivo
In vivo Eplerenone inhibits upregulated phosphorylation of PKCepsilon, MAP kinase, and p90RSK in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone increases downregulated endothelial nitric oxide synthase mRNA in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone administration results in significant improvement in glomerulosclerosis and urinary protein in DS rats. [1] Eplerenone (200 mg/kg/day) administration significantly decreases systolic and diastolic blood pressure by 12% and 11%, respectively, compared with untreated mice. Eplerenone increases serum susceptibility to lipid peroxidation decreased by as much as 26%, and serum paraoxonase activity in mice. Eplerenone significantly reduces the atherosclerotic lesion area in aortas of mice, and this effect is reversed by AT-II. [2] Eplerenone increases total vessel area by 30% and luminal area by nearly 60% compared with the no-treatment group, without affecting neointima size in pigs. [3] Eplerenone significantly decreases LV end-diastolic wall stress in dogs. Eplerenone is associated with a 28% reduction in cardiomyocyte cross-sectional area, a 37% reduction of volume fraction of reactive interstitial fibrosis, and a 34% reduction of volume fraction of replacement fibrosis in dogs with heart failure. [4] Eplerenone blunts the increase in pulse pressure in Aldo rats and normalized Einc-wall stress curves, medial cross-sectional area (MCSA), and EIIIA fibronectin in aldosterone (Aldo)-salt hypertensive rats. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06168994 Not yet recruiting
Paroxysmal Atrial Fibrillation
Assiut University
 February 1 2024 Phase 4
NCT06208072 Recruiting
Primary Hypertension|Obesity
Hippocration General Hospital|National and Kapodistrian University of Athens
 September 1 2023 Not Applicable

Chemical Information & Solubility

Molecular Weight 414.49 Formula

C24H30O6
CAS No. 107724-20-9 SDF Download Eplerenone SDF
Smiles CC12CCC(=O)C=C1CC(C3C24C(O4)CC5(C3CCC56CCC(=O)O6)C)C(=O)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 10 mg/mL ( (24.12 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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