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[CAS NO. 107724-20-9] Eplerenone

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Catalog:	HY-B0251
Brand:	MCE
CAS:	107724-20-9

Overview

MDL	-
Molecular Weight	414.49
Molecular Formula	C24H30O6
SMILES	O=C(CC1)O[C@@]21CC[C@@]3([H])[C@]4([H])[C@H](C(OC)=O)CC5=CC(CC[C@]5(C)[C@@]46[C@H](O6)C[C@@]32C)=O

For research use only. We do not sell to patients.

4 Publications Citing Use of MCE

[1]Br J Pharmacol. 2021 Aug;178(15):2976-2997.
[2]J Pharmaceut Biomed. 2020, 113870.
[3]Mol Med Rep. 2020 Sep;22(3):1859-1867.
[4]Research Square Preprint. 2021 Apr.

Summary

Eplerenone (Epoxymexrenone) is a selective, highly specific and orally active aldosterone blocker (SAB). Eplerenone also is a selective mineralocorticoid receptor antagonist (MRA) with IC ₅₀ value of 0.081 μM. Eplerenone can be used for the research of hypertension, atherosclerosis, chronic systolic heart failure (HF) and cardiovascular (CV) ^[1] ^[2] .

IC50 & Target

IC50: 0.081 μM (human mineralocorticoid receptor) ^[2]

In Vitro

Eplerenone inhibits the human mineralocorticoid receptor with IC ₅₀ value of 0.081 μM ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Eplerenone (oral, 200 mg/kg/day for 3 months) significantly reduces oxidative stress and atherosclerosis progression in atherosclerotic apolipoprotein edeficient (EO) mice ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Atherosclerotic apolipoprotein Edeficient (EO) mice ^[3]
Dosage:	200 mg/kg
Administration:	oral, 200 mg/kg/day for 3 months
Result:	Significantly decreased systolic and diastolic blood pressure by 12% and 11%, respectively. Decreased serum susceptibility to lipid peroxidation by as much as 26%, and increased serum paraoxonase activity by 28%. Reduced levels of lipid peroxides, and significantly reduced macrophage oxidation of low-density lipoprotein (LDL) and superoxide ion release. Significantly reduced the atherosclerotic lesion area.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00430924	Lene Boesby\|Rigshospitalet, Denmark\|Herlev Hospital	Kidney Failure, Chronic	March 2007	Phase 4
NCT01996449	University of Texas Southwestern Medical Center	Hypertension	July 2013	Phase 2
NCT00391846	AstraZeneca	Heart Failure\|Ventricular Dysfunction, Left	October 2006	Phase 4
NCT01893788	Nagoya University	Hypertensive Left Ventricular Hypertrophy	April 2013	Phase 4
NCT02345590	Bayside Health\|Baker Heart and Diabetes Institute	Aortic Aneurysm, Abdominal	May 2015	Phase 4
NCT03342690	Pfizer´s Upjohn has merged with Mylan to form Viatris Inc.\|Pfizer	Chronic Heart Failure	July 5, 2017
NCT00608465	Vanderbilt University\|Vanderbilt University Medical Center	Metabolic Syndrome X	May 2006	Phase 4
NCT00505336	St Vincent´s University Hospital, Ireland	Diastolic Heart Failure	April 2006	Not Applicable
NCT01794091	Brigham and Women´s Hospital	Diabetes Mellitus, Type II	August 2013	Phase 1
NCT02871648	Brigham and Women´s Hospital	Healthy Volunteers	January 2016	Phase 1
NCT02809963	Herlev Hospital	Diabetes Type 2	November 2015	Phase 4
NCT01650012	McMaster University\|Canadian Institutes of Health Research (CIHR)	Hemodialysis\|End Stage Renal Disease	March 2013	Not Applicable
NCT01405456	Massachusetts General Hospital	HIV	January 2012	Not Applicable
NCT00825188	University of Mississippi Medical Center	Obesity\|Hypertension	January 2009	Not Applicable
NCT04300881	Wagner Macula & Retina Center\|ThromboGenics	Vitreomacular Traction\|Subretinal Edema	October 4, 2019	Phase 2
NCT00647192	University Hospital, Saarland\|University Medical Center Groningen\|Pfizer	Atrial Fibrillation	March 2008	Phase 2
NCT02462499	Semmelweis University	Chronic Central Serous Chorioretinopathy	June 2014	Phase 4
NCT01955694	Bayer	Heart Failure	November 11, 2013	Phase 2
NCT02118753	Radboud University Medical Center	Ischemia-reperfusion Injury	March 2014	Not Applicable
NCT01837108	Radboud University Medical Center	Pharmacodynamics	April 2013	Phase 4
NCT05198791	NHS National Waiting Times Centre Board\|British Heart Foundation\|Abbott	Myocardial Infarction, Acute\|Myocardial Infarction With Nonobstructive Coronary Arteries\|Myocardial Injury	February 4, 2022	Phase 2
NCT02345044	Daiichi Sankyo, Inc.	Essential Hypertension	January 2015	Phase 2
NCT00553722	Shaare Zedek Medical Center	Hypertension\|Dialysis\|Hyperaldosteronism	November 2007	Phase 4
NCT01801228	Emma Nilsson\|Göteborg University\|Uppsala University Hospital\|Karolinska University Hospital\|University Hospital, Linkoeping\|University Hospital, Umeå\|Region Örebro County\|Region Skane	Ascites\|Cirrhosis	February 2013	Phase 2
NCT02153125	Tel-Aviv Sourasky Medical Center	Central Serous Chorioretinopathy	April 2014	Phase 2
NCT03165240	Boehringer Ingelheim	Diabetic Nephropathies	October 5, 2017	Phase 1
NCT02740179	Massachusetts General Hospital	HIV	January 2017	Not Applicable
NCT02890173	Daiichi Sankyo Co., Ltd.\|Daiichi Sankyo, Inc.	Essential Hypertension	September 2016	Phase 3
NCT00980031	Creighton University	Myocardial Remodeling	April 2007	Not Applicable
NCT03923530	North Florida Foundation for Research and Education\|Malcom Randall VA Medical Center	Hypertension\|Aortic Stenosis, Calcific\|Quality of Life\|Heart Failure With Preserved Ejection Fraction	June 3, 2019	Early Phase 1
NCT00147615	Pfizer´s Upjohn has merged with Mylan to form Viatris Inc.\|Pfizer	Hypertension	October 2004	Phase 3
NCT01176968	Pfizer´s Upjohn has merged with Mylan to form Viatris Inc.\|Pfizer	Myocardial Infarction	September 2010	Phase 4
NCT01100203	Lene Boesby\|Rigshospitalet, Denmark\|Herlev Hospital	Chronic Kidney Disease	April 2010	Phase 3
NCT00147589	Pfizer´s Upjohn has merged with Mylan to form Viatris Inc.\|Pfizer	Hypertension	September 2004	Phase 3
NCT00865176	Sandoz	Hypertension	June 2006	Phase 1
NCT01319344	University of Erlangen-Nürnberg Medical School	Metabolic Syndrome\|Endothelial Dysfunction	September 2010	Phase 3
NCT01275352	Washington University School of Medicine\|University of Pennsylvania	Hypertension	December 2011	Phase 4
NCT00214825	Brigham and Women´s Hospital\|National Institutes of Health (NIH)	Diabetes Mellitus\|Endothelial Dysfunction\|Albuminuria	August 2003	Not Applicable
NCT00407784	Erasmus Medical Center\|Dutch Kidney Foundation\|Pfizer	Hyperaldosteronism\|Hypertension	January 2007
NCT02957435	Biolab Sanus Farmaceutica	Pharmacokinetics\|Healthy Subjects\|Fasting	July 2017	Phase 1
NCT01708798	University of British Columbia\|Canadian Cancer Society (CCS)\|Pfizer	Breast Cancer	May 2014	Phase 2\|Phase 3
NCT00865618	Sandoz	Hypertension	June 2006	Phase 1
NCT05030545	Brigham and Women´s Hospital	Primary Aldosteronism\|Hypertension	October 2021	Phase 4
NCT04840342	Brigham and Women´s Hospital	Hypertension\|Mineralocorticoid Excess	February 3, 2022	Phase 4
NCT01990677	Wills Eye\|Mid Atlantic Retina	Central Serous Chorioretinopathy	October 2013	Not Applicable
NCT00649311	Pfizer	Hypertension	April 2003	Phase 2
NCT05104138	Federico II University	Central Serous Chorioretinopathy	October 1, 2015
NCT00082589	Pfizer´s Upjohn has merged with Mylan to form Viatris Inc.\|Pfizer	Heart Failure, Congestive	April 2004	Phase 4
NCT03683069	Brigham and Women´s Hospital	Hypertension\|Genetics Hypertension	January 15, 2019	Phase 4
NCT01473108	Bayer	Clinical Pharmacology	March 29, 2010	Phase 1
NCT03017703	University of Southern Denmark	Endothelial Dysfunction\|Insulin Resistance	December 1, 2016	Not Applicable
NCT01115855	Pfizer´s Upjohn has merged with Mylan to form Viatris Inc.\|Pfizer	Heart Failure	July 2010	Phase 3
NCT01427972	Eli Lilly and Company	Chronic Kidney Disease	September 2011	Phase 2
NCT01394627	Brigham and Women´s Hospital\|Robert Wood Johnson Foundation\|National Institutes of Health (NIH)\|National Heart, Lung, and Blood Institute (NHLBI)	Hypoglycemia	January 2011	Not Applicable
NCT00315016	Radboud University Medical Center	Diabetic Nephropathy	January 2007	Phase 2
NCT00147563	Pfizer	Hypertension	October 2003	Phase 4
NCT03984591	Bispebjerg Hospital\|Rigshospitalet, Denmark	Systolic Heart Failure	November 1, 2020	Phase 4
NCT01834768	CHU de Reims\|Institut National de la Santé Et de la Recherche Médicale, France	Chronic Kidney Insufficiency\|Kidney Transplantation	February 2013	Phase 2
NCT02490904	Central Hospital, Nancy, France	End-stage Renal Disease	October 19, 2016	Phase 3
NCT00232180	Pfizer´s Upjohn has merged with Mylan to form Viatris Inc.\|Pfizer	Heart Failure	March 2006	Phase 3
NCT02525796	Brigham and Women´s Hospital	Primary Hyperparathyroidism	January 2016	Phase 2\|Phase 3
NCT01887119	Maastricht University Medical Center	Abdominal Obesity Metabolic Syndrome\|Insulin Resistance\|Hypertension	October 2013	Phase 4
NCT00138944	University of Erlangen-Nürnberg Medical School	Essential Hypertension	January 2007	Phase 3
NCT00108251	US Department of Veterans Affairs\|VA Office of Research and Development	Congestive Heart Failure\|Diastole	August 2004	Phase 4
NCT00223717	Vanderbilt University\|Vanderbilt University Medical Center	Hypertension	January 2001	Phase 1
NCT04519164	Brigham and Women´s Hospital	Metabolic Syndrome\|Hypertension\|Overweight and Obesity	December 1, 2020	Phase 4
NCT00132093	NHS Greater Glasgow and Clyde	Myocardial Infarction	April 2005	Phase 4
NCT04697485	Northwestern University	HF - Heart Failure\|Diabetes Mellitus	January 8, 2021	Phase 4
NCT01971593	Washington University School of Medicine\|Pfizer	Tetralogy of Fallot\|Transposition of the Great Vessels With an Arterial Switch\|Single Ventricle With a Fontan Palliation	August 2013	Phase 4
NCT05593055	Brigham and Women´s Hospital	Hypertension\|Left Ventricular Hypertrophy	April 2023	Phase 4
NCT00401856	Royal Brompton & Harefield NHS Foundation Trust	Cardiomyopathy	December 2007	Phase 4
NCT00990223	Pfizer´s Upjohn has merged with Mylan to form Viatris Inc.\|Pfizer	Healthy Volunteers	October 2009	Phase 1
NCT04746495	University of Michigan\|National Heart, Lung, and Blood Institute (NHLBI)	Hypertension	October 2022	Phase 4
NCT03418649	University of Cincinnati	Degenerative Intervertebral Discs\|Sciatic Radiculopathy\|Low Back Pain	July 2022	Phase 4
NCT01786551	Brigham and Women´s Hospital	Systemic Proinflammatory State	March 2010	Not Applicable
NCT03079141	Leiden University Medical Center\|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)\|Radboud University Medical Center	Chronic Central Serous Chorioretinopathy	February 20, 2017	Phase 4
NCT01586442	Montreal Heart Institute\|Pfizer	Heart Failure\|Type 2 Diabetes\|Glucose Intolerance	March 2012	Phase 3
NCT00515021	Vanderbilt University Medical Center\|National Center for Research Resources (NCRR)	Metabolic Syndrome X	April 2007	Phase 4
NCT00703352	Hospital Universitari Vall d´Hebron Research Institute\|Pfizer	Transposition of Great Vessels\|Atrial Switch Procedure	July 2008	Phase 4
NCT00817635	Novartis\|Great Lakes Drug Development, Inc.\|Integrium	Hypertension	December 22, 2008	Phase 2
NCT01807221	Bayer	Heart Failure	June 17, 2013	Phase 2
NCT00758524	Novartis Pharmaceuticals\|Novartis	Essential Hypertension	September 11, 2008	Phase 2
NCT02607657	Biolab Sanus Farmaceutica	Healthy Volunteers	May 2016	Phase 1
NCT02354352	Ohio State University\|University of California, Los Angeles\|University of Utah\|University of Colorado, Denver\|University of Kansas Medical Center\|Vanderbilt University Medical Center	Duchenne Muscular Dystrophy	March 20, 2015	Phase 3
NCT00293150	The Cleveland Clinic	Diastolic Heart Failure	September 2003	Phase 4
NCT01302236	Jichi Medical University	Hypertension\|Chronic Kidney Disease.	March 2011	Phase 4
NCT03476616	Hippocration General Hospital	Hypertension\|Obesity	September 1, 2018	Phase 4
NCT03186742	Poznan University of Medical Sciences	Hypertension,Essential\|Obstructive Sleep Apnea\|Left Ventricular Hypertrophy	July 1, 2014	Phase 4
NCT01521546	Subha Raman\|Ballou Skies\|Ohio State University	Duchenne Muscular Dystrophy	February 2012	Not Applicable
NCT02215330	Prim. Prof. Dr. Oliver Findl, MBA\|Vienna Institute for Research in Ocular Surgery	Central Serous Chorioretinopathy	October 2014	Phase 2\|Phase 3
NCT00187889	University of Florida\|National Heart, Lung, and Blood Institute (NHLBI)\|Pfizer	Ischemic Heart Disease	August 2004	Phase 4
NCT04450953	Pr. Nicolas GIRERD\|Central Hospital, Nancy, France	Kidney Transplantation for More Than One Year\|Patients With a Kidney Transplantation on Cyclosporine	October 12, 2021	Phase 3
NCT01373086	Novartis Pharmaceuticals\|Novartis	Hypertension	May 2011	Phase 2
NCT01857856	M.p. van den Berg, MD, PhD, professor in Cardiology\|University Medical Center Groningen\|The Interuniversity Cardiology Institute of the Netherlands\|ZonMw: The Netherlands Organisation for Health Research and Development\|Netherlands: CVON, CardioVascular Research Netherlands	Phospholamban R14del Mutation-related Cardiomyopathy	May 2013	Phase 3
NCT01822561	Tufts Medical Center	Central Serous Chorioretinopathy	May 2013	Phase 2
NCT01237899	Eli Lilly and Company	Chronic Kidney Disease	October 2010	Phase 1
NCT01832558	Medical University of Vienna	CKD II-III	November 2012	Not Applicable

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 60.32 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4126 mL	12.0630 mL	24.1260 mL
5 mM	0.4825 mL	2.4126 mL	4.8252 mL
10 mM	0.2413 mL	1.2063 mL	2.4126 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Myron H Weinberger, et al. Eplerenone, a selective aldosterone blocker, in mild-to-moderate hypertension. Am J Hypertens. 2002 Aug;15(8):709-16.
[2] Dhillon, S., Eplerenone: a review of its use in patients with chronic systolic heart failure and mild symptoms. Drugs, 2013. 73(13): p. 1451-62.
[3] Shlomo Keidar, et al. Effect of eplerenone, a selective aldosterone blocker, on blood pressure, serum and macrophage oxidative stress, and atherosclerosis in apolipoprotein E-deficient mice. J Cardiovasc Pharmacol. 2003 Jun;41(6):955-63.

Synonyms

Pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo-, γ-lactone, 7-methyl ester, (7α,11α,17α)-

Pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo-, γ-lactone, methyl ester, (7α,11α,17α)-

Spiro[9,11-epoxy-9H-cyclopenta[a]phenanthrene-17(2H),2′(3′H)-furan], pregn-4-ene-7,21-dicarboxylic acid deriv.

CGP 30083

SC 66110

Eplerenone

SC 6110

Epoxymexrenone

Inspra

Selara

(+)-Eplerenone

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