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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Choose Selective Glucocorticoid Receptor Inhibitors

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 MX;GeY5kfGmxbjDhd5NigQ>? M3noZWFvfGGpb37pd5Qh[WO2aY\peJkh[XRiR3HsOE11[WepZXSgcYlv\XKjbH;jc5J1cWOxaXSgdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKGi3bXHuJGh2cDdiY3XscJMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyPUCuNVIzKM7:TR?= Mn60NlA3PzJ6MkK=
COS1 cells M1vPbGZ2dmO2aX;uJIF{e2G7 MnLJNUBl[Xm| M3;uRWFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4hVVJidILhcpNn\WO2ZXSgbY4hcHWvYX6gR29UOSClZXzsd{Bi\nSncjCxJIRigSCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9NU4{KM7:TR?= MXmyNlA4PDF2Mh?=
293 cells MX\GeY5kfGmxbjDhd5NigQ>? NH;JeYoyPiCq NIf4SZNFcXOybHHj[Y1mdnRib3[gX|NJZWGuZH;zeIVzd26nIH\yc40hcHWvYX6gcYlv\XKjbH;jc5J1cWOxaXSgdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKDJ7MzDj[YxteyCjZoTldkAyPiCqcoOgZpkhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygTWM2OD1{Lk[g{txO MnrqNlUyQDd{N{e=

... 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
Synonyms CGP 30083, SC-66110

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02957435 Not yet recruiting Pharmacokinetics|Healthy Subjects|Fasting Biolab Sanus Farmaceutica June 2017 Phase 1
NCT02740179 Recruiting HIV Massachusetts General Hospital January 2017 --
NCT03017703 Recruiting Endothelial Dysfunction|Insulin Resistance University of Southern Denmark December 2016 --
NCT02890173 Recruiting Essential Hypertension Daiichi Sankyo Co., Ltd.|Daiichi Sankyo Inc. September 2016 Phase 3
NCT02607657 Withdrawn Healthy Volunteers Biolab Sanus Farmaceutica May 2016 Phase 1
NCT02525796 Recruiting Primary Hyperparathyroidism Brigham and Womens Hospital January 2016 Phase 2|Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID