Eplerenone

Catalog No.S1707 Synonyms: CGP 30083, SC-66110

Eplerenone Chemical Structure

Molecular Weight(MW): 414.49

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

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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]
()
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Huh7 cells M3fYOGZ2dmO2aX;uJIF{e2G7 M{XIUmFvfGGpb37pd5Qh[WO2aY\peJkh[XRiR3HsOE11[WepZXSgcYlv\XKjbH;jc5J1cWOxaXSgdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKGi3bXHuJGh2cDdiY3XscJMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyPUCuNVIzKM7:TR?= NETxbnAzODZ5MkiyNi=>
COS1 cells MUDGeY5kfGmxbjDhd5NigQ>? M3zT[FEh\GG7cx?= MnrNRY51[WexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBOWiC2cnHud4Zm[3SnZDDpckBpfW2jbjDDU3MyKGOnbHzzJIFnfGW{IEGg[IF6KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhUUN3ME2xMlMh|ryP NHnEXG0zOjB5NEG0Ni=>
293 cells M1XyWWZ2dmO2aX;uJIF{e2G7 MorXNVYhcA>? MnPNSIl{eGyjY3Xt[Y51KG:oIGuzTH1idGSxc4Tldo9v\SCocn;tJIh2dWGwIH3pcoVz[WyxY3;yeIlkd2mmIILlZ4VxfG:{IHX4dJJme3OnZDDpckAzQTNiY3XscJMh[W[2ZYKgNVYhcHK|IHL5JJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFnDOVA:Oi54IN88US=> NIe0XGUzPTF6N{K3Oy=>

... Click to View More Cell Line Experimental Data

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]

Protocol

Solubility (25°C)

In vitro DMSO 4 mg/mL warmed (9.65 mM)
Water Insoluble
Ethanol Insoluble

* 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 414.49
Formula

C24H30O6

CAS No. 107724-20-9
Storage powder
in solvent
Synonyms CGP 30083, SC-66110

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02215330 Unknown status Drug: Eplerenone|Drug: Maltodextrin Central Serous Chorioretinopathy Prim. Prof. Dr. Oliver Findl MBA|Vienna Institute for Research in Ocular Surgery October 2014 Phase 2|Phase 3
NCT03186742 Completed Drug: Eplerenone 50 mg Tab HypertensionEssential|Obstructive Sleep Apnea|Left Ventricular Hypertrophy Poznan University of Medical Sciences July 1 2014 Phase 4
NCT02462499 Completed Drug: Inspra (eplerenone) Chronic Central Serous Chorioretinopathy Semmelweis University June 2014 Phase 4
NCT02118753 Completed Drug: Eplerenone Ischemia-reperfusion Injury Radboud University March 2014 Not Applicable

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID