Cat. No.: HY-B0251

Eplerenone

(Synonyms: Epoxymexrenone)

8 Cited Publications

Customer Review

Based on 8 publication(s) in Google Scholar

Eplerenone (Epoxymexrenone) is a selective, highly specific and orally active aldosterone blocker (SAB). Eplerenone also is a selective mineralocorticoid receptor antagonist (MRA) with IC₅₀ value of 0.081 μM. Eplerenone can be used for the research of hypertension, atherosclerosis, chronic systolic heart failure (HF) and cardiovascular (CV).

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

Purity: 99.81%
CAS No.: 107724-20-9
Formula: C₂₄H₃₀O₆
Molecular Weight:414.49

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Eplerenone Chemical Structure

CAS No.: 107724-20-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

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

All Endogenous Metabolite Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A10	IC₅₀	>5000 nM Compound: 1	Inhibition of L-type calcium channel in rat A10 cells assessed as inhibition of depolarization-induced increase in calcium flux after 48 hrs by FLIPR assay Inhibition of L-type calcium channel in rat A10 cells assessed as inhibition of depolarization-induced increase in calcium flux after 48 hrs by FLIPR assay	[PMID: 20408553]
COS-1	IC₅₀	1300 nM Compound: Eplerenone	Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay	[PMID: 22074142]
COS-1	IC₅₀	1300 nM Compound: Eplerenone	Antagonist activity at human mineralocorticoid receptor expressed in COS1 cells after 1 day by luciferase reporter gene assay Antagonist activity at human mineralocorticoid receptor expressed in COS1 cells after 1 day by luciferase reporter gene assay	[PMID: 25187277]
HEK293	IC₅₀	2600 nM Compound: Eplerenone	Displacement of [3H]aldosterone from cytosolic human MR expressed in HEK293 cells after 16 hrs by scintillation counting Displacement of [3H]aldosterone from cytosolic human MR expressed in HEK293 cells after 16 hrs by scintillation counting	[PMID: 22074142]
Huh-7	IC₅₀	135 nM Compound: 1	Antagonist activity at Gal4-fused mineralocorticoid receptor expressed in human HuH7 cells assessed as inhibition of aldosterone-induced receptor activation by luciferase reporter gene assay Antagonist activity at Gal4-fused mineralocorticoid receptor expressed in human HuH7 cells assessed as inhibition of aldosterone-induced receptor activation by luciferase reporter gene assay	[PMID: 20408553]
Huh-7	IC₅₀	122 nM Compound: 1	Antagonist activity at mineralocorticoid receptor LBD expressed in human HUH7 cells coexpressing GAL4 by luciferase reporter gene assay Antagonist activity at mineralocorticoid receptor LBD expressed in human HUH7 cells coexpressing GAL4 by luciferase reporter gene assay	[PMID: 20672820]
Huh-7	IC₅₀	122 nM Compound: eplerenone	Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay	[PMID: 20672822]

In Vitro

Eplerenone inhibits the human mineralocorticoid receptor with IC₅₀ value of 0.081 μM^[2].

MedChemExpress (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].

MedChemExpress (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 A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 107724-20-9
Appearance Solid
Molecular Weight 414.49
Formula C₂₄H₃₀O₆
Color White to off-white
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
Synonyms

Epoxymexrenone
Structure Classification
- Steroids
Initial Source
- Endogenous metabolite
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

All Histological Imaging/StainingWBCell Imaging/StainingCell Proliferation/Viability AssayFlow Cytometry

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Journal Impact Factor

Br J Pharmacol

Protopanaxadiol alleviates neuropathic pain by spinal microglial dynorphin A expression following glucocorticoid receptor activation. [Abstract]

2021 Aug;178(15):2976-2997. PMID: 33786848
Biochem Pharmacol

Tspan4+ fibroblasts facilitate the development of NECSO in myocardial ischemia reperfusion through migrasomes-mediated Tnf-α autocrine and cardiomyocytes aldosterone generation. [Abstract]

2026 Mar 24:249:117928. PMID: 41887336
Sci Rep

Activation/inactivation of Tregs mediated by Kv1.3 potassium channels synergistically with exosome secretion to regulate myocardial fibrosis. [Abstract]

2025 Dec 1;15(1):45756. PMID: 41326524

Eplerenone purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Dec 1;15(1):45756. [Abstract]

Eplerenone (200 mg/kg/day). Hematoxylin and eosin (H&E) staining was performed to assess cardiomyocyte arrangement and inflammatory infiltration.
Mol Med Rep

Age‑related changes in mineralocorticoid receptors in rat hearts. [Abstract]

2020 Sep;22(3):1859-1867. PMID: 32582979

Eplerenone purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2020 Sep;22(3):1859-1867. [Abstract]

Eplerenone (1 μM). Mmunoblotting and semi-quantification of p16, p21, p53 and NADP subunits, p47-phox, p67-phox and gp91-phox expression in H9C2 cells. Protein expression levels were normalized to GAPDH.
J Pharm Biomed Anal

Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]

2021 Feb 20:195:113870. PMID: 33453569
Theriogenology

Aldosterone regulates in vitro maturation of porcine oocytes derived from small follicles via Wnt/ β-catenin. [Abstract]

2026 Apr 15:255:117836. PMID: 41564797

Eplerenone purchased from MedChemExpress. Usage Cited in: Theriogenology. 2026 Apr 15:255:117836. [Abstract]

Representative images of cumulus cell expansion and oocytes with or without polar bodies in the control group and groups treated with different concentrations of EPL (Eplerenone) after in vitro maturation (IVM).
Otol Neurotol

Cortisol Sensitizes Cochlear Hair Cells to Gentamicin Ototoxicity Via Endogenous Apoptotic Pathway. [Abstract]

2024 Jan 1;45(1):e49-e56. PMID: 38085767

Eplerenone purchased from MedChemExpress. Usage Cited in: Otol Neurotol. 2024 Jan 1;45(1):e49-e56. [Abstract]

Cells were treated with cortisol (50 μmol/l) in combination with different concentrations of RU486 or Eplerenone for 24 hours.

Eplerenone purchased from MedChemExpress. Usage Cited in: Otol Neurotol. 2024 Jan 1;45(1):e49-e56. [Abstract]

HEI-OC1 cells were treated with 50 μmol/l cortisol in combination with 0.1 nmol/l RU486 or 1 μmol/l Eplerenone for 24 hours and then treated with 50 mmol/l GM for 24 hours. apoptosis was assessed by flow cytometry using Annexin V and PI staining kit.
Research Square Preprint

2021 Apr.

Solvent & Solubility

In Vitro:

DMSO : 23.33 mg/mL (56.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4126 mL	12.0630 mL	24.1260 mL	60.3151 mL
	5 mM	0.4825 mL	2.4126 mL	4.8252 mL	12.0630 mL
	10 mM	0.2413 mL	1.2063 mL	2.4126 mL	6.0315 mL
	15 mM	0.1608 mL	0.8042 mL	1.6084 mL	4.0210 mL
	20 mM	0.1206 mL	0.6032 mL	1.2063 mL	3.0158 mL
	25 mM	0.0965 mL	0.4825 mL	0.9650 mL	2.4126 mL
	30 mM	0.0804 mL	0.4021 mL	0.8042 mL	2.0105 mL
	40 mM	0.0603 mL	0.3016 mL	0.6032 mL	1.5079 mL
	50 mM	0.0483 mL	0.2413 mL	0.4825 mL	1.2063 mL

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Eplerenone

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Publications Citing Use of MedChemExpress (MCE) Eplerenone

All Endogenous Metabolite Isoforms

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Eplerenone Related Classifications

Cat. No.: HY-B0251