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|
|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|
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