Eplerenone
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).
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- Pureza : 99.81%
- No. CAS: 107724-20-9
- Fòrmula: C24H30O6
- Peso molecular:414.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Eplerenone
More- Br J Pharmacol. 2021 Aug;178(15):2976-2997. [Abstract]
- Biochem Pharmacol. 2026 Jul:249:117928. [Abstract]
- Mol Med Rep. 2020 Sep;22(3):1859-1867. [Abstract]
- Sci Rep. 2025 Dec 1;15(1):45756. [Abstract]
- J Pharm Biomed Anal. 2021 Feb 20:195:113870. [Abstract]
- Theriogenology. 2026 Apr 15:255:117836. [Abstract]
- Otol Neurotol. 2024 Jan 1;45(1):e49-e56. [Abstract]
- Research Square Preprint. 2021 Apr.
Customer Validation & Images
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Cell Imaging/Staining
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Histological Imaging/Staining
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Cell Proliferation/Viability Assay
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Flow Cytometry
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WB
Ver todos los productos específicos de isoformas Endogenous Metabolite
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 0.081 μM (human mineralocorticoid receptor) [2]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A10 | IC50 |
>5000 nM
Compound: 1
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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
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[PMID: 20408553] |
| COS-1 | IC50 |
1300 nM
Compound: Eplerenone
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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
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[PMID: 22074142] |
| COS-1 | IC50 |
1300 nM
Compound: Eplerenone
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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
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[PMID: 25187277] |
| HEK293 | IC50 |
2600 nM
Compound: Eplerenone
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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
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[PMID: 22074142] |
| Huh-7 | IC50 |
135 nM
Compound: 1
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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
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[PMID: 20408553] |
| Huh-7 | IC50 |
122 nM
Compound: 1
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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
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[PMID: 20672820] |
| Huh-7 | IC50 |
122 nM
Compound: eplerenone
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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
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[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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Atherosclerotic apolipoprotein Edeficient (EO) mice[3]
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Dosage:200 mg/kg
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Administration:oral, 200 mg/kg/day for 3 months
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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.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 107724-20-9
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Appearance Solid
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Peso molecular 414.49
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Fòrmula C24H30O6
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Color White to off-white
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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
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Synonyms
Epoxymexrenone
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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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 Jul:249:117928. PMID: 41887336 -
Mol Med Rep
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.
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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.
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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).
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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.
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Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
Pureza y Documentación
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Ficha de datos (295 KB)
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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)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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 |
Eplerenone Related Classifications
HY-B0251 Related Classifications
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