2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. Mineralocorticoid Receptor Endogenous Metabolite
  4. Eplerenone

Eplerenone  (Synonyms: Epoxymexrenone)

Cat. No.: HY-B0251 Purity: 99.71%
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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.

Eplerenone Chemical Structure

Eplerenone Chemical Structure

CAS No. : 107724-20-9

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 97 In-stock
Solid
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10 mg USD 88 In-stock
50 mg USD 259 In-stock
100 mg USD 354 In-stock
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Based on 5 publication(s) in Google Scholar

Other Forms of Eplerenone:

Eplerenone Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)[1][2].

IC50 & Target

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

Eplerenone Related Antibodies
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
Molecular Weight

414.49

Formula

C24H30O6
CAS No.
Appearance

Solid

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
Structure Classification
Initial Source
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
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (60.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* 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

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
60 mM 0.0402 mL 0.2011 mL 0.4021 mL 1.0053 mL
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Eplerenone Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Eplerenone107724-20-9EpoxymexrenoneMineralocorticoid ReceptorEndogenous Metabolitealdosteronespecificmineralocorticoid receptorMRAhypertensionchronic systolic heart failure (HF)cardiovascular (CV)atherosclerosisInhibitorinhibitorinhibit

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