Catalog No.S1707 Synonyms: CGP 30083, SC-66110
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
|Description||Eplerenone is a mineralocorticoid receptor antagonist, and blocks the action of aldosterone, used to control high blood pressure.|
|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.  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.  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.  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.  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. |
-  Kobayashi N, et al. Hypertension, 2005, 45(4), 538-544.
-  Keidar S, et al. J Cardiovasc Pharmacol, 2003, 41(6), 955-963.
-  Ward MR, et al. Circulation, 2001, 104(4), 467-472.
|In vitro||DMSO||4 mg/mL warmed (9.65 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.
|Synonyms||CGP 30083, SC-66110|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03165240||Recruiting||Diabetic Nephropathies||Boehringer Ingelheim||October 5 2017||Phase 1|
|NCT03342690||Recruiting||Chronic Heart Failure||Pfizer||July 5 2017||--|
|NCT02957435||Withdrawn||Pharmacokinetics|Healthy Subjects|Fasting||Biolab Sanus Farmaceutica||July 2017||Phase 1|
|NCT02740179||Recruiting||HIV||Massachusetts General Hospital||January 2017||Not Applicable|
|NCT03017703||Recruiting||Endothelial Dysfunction|Insulin Resistance||University of Southern Denmark||December 2016||Not Applicable|
|NCT02490904||Recruiting||End-stage Renal Disease||Central Hospital Nancy France||October 2016||Phase 3|
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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