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Fig. 1 · Structure
Cat. No.
A10358
CAS No.
107724-20-9
Formula
C24H30O6
Mol. Weight
414.49

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Eplerenone

Aldosterone Blocker

Eplerenone is a selective and highly specific aldosterone blocker, functioning as a mineralocorticoid receptor antagonist with an IC50 of 0.081 µM. This compound is utilized in research focused on hypertension, atherosclerosis, chronic systolic heart failure, and various cardiovascular conditions. Eplerenone’s ability to effectively inhibit aldosterone activity makes it an important tool in studying the mechanisms underlying these diseases and in the development of therapeutic strategies.

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Biological Activity

Bioactivity / Mechanism

Eplerenone bound human mineralocorticoid receptor in a competition assay (pKi 7.0 ± 0.1, SD; n = 10 observations). Lower affinities were reported for the other steroid receptors in the tested panel. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

In Vitro Studies

In U2-OS cells expressing full-length human MR, eplerenone fully antagonized aldosterone-driven reporter activation (IC50 0.34 μM) and was inactive without aldosterone. This is a functional assay endpoint, not a treatment dose. [1]

Steroid receptor competition binding

Biochemical assay · Recombinant human MR ligand-binding domain; human GR, PR and AR ligand-binding domains [1]

Eplerenone competed in steroid receptor radioligand-binding assays, with the highest reported affinity in this panel at MR.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
MR ligand-binding affinitypKi 7.0 ± 0.1 (SD; n = 10 observations)[1]
GR ligand-binding affinitypKi 4.9 ± 0.1 (SD; n = 3 observations)[1]
PR ligand-binding affinitypKi 4.3 ± 0.2 (SD; n = 3 observations)[1]
AR ligand-binding affinitypKi 5.3 ± 0.3 (SD; n = 3 observations)[1]

Literature-Reported Treatment Conditions

Method
Scintillation-proximity MR competition assay with aldosterone radioligand; filtration assays for GR, PR and AR.
Reported limits
Main ligand-binding methods refer to an earlier protocol that was not retrieved. Assay concentration series, incubation time and assay-specific eplerenone supplier/purity are not specified in the read main-text methods.
Methods and source locations

Compound reported in the paper: Eplerenone; Compound label in the paper: eplerenone

Published experiments with eplerenone; no Adooq supplier, lot, purity or formulation equivalence is established.

Materials and methods: Ligand binding assays; Results: AZD9977 is a partial MR antagonist in vitro; Table 1 and footnote; Fig. 1

MR ligand-binding affinity: Competition binding; Table 1 defines ± as standard deviation and n as number of observations. — Table 1, eplerenone MR row and table footnote; Ligand binding assays

GR ligand-binding affinity: Competition binding; Table 1 defines ± as standard deviation and n as number of observations. — Table 1, eplerenone GR row and table footnote; Ligand binding assays

PR ligand-binding affinity: Competition binding; Table 1 defines ± as standard deviation and n as number of observations. — Table 1, eplerenone PR row and table footnote; Ligand binding assays

AR ligand-binding affinity: Competition binding; Table 1 defines ± as standard deviation and n as number of observations. — Table 1, eplerenone AR row and table footnote; Ligand binding assays

Human MR functional antagonism

Cell-based study · U2-OS cells expressing full-length human MR with an MMTV-luciferase reporter [1]

Eplerenone fully antagonized aldosterone-driven reporter activation and showed no agonist activity when tested without aldosterone in this assay.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Inhibition of aldosterone-activated full-length human MR reporterIC50 0.34 μM[1]
MR reporter activation without aldosteroneAgonist activity Inactive in this assay[1]

Literature-Reported Treatment Conditions

Treatment concentration
Concentration-response series; 0.1 nM aldosterone in the antagonist condition.
Exposure duration
24 hours
Method
Addition in cell medium followed by luciferase luminescence measurement.
Co-treatment
Aldosterone challenge; a separate condition omitted aldosterone.
Reported limits
Assay-specific eplerenone supplier/purity and solvent are not specified in the read reporter methods.
Methods and source locations

Compound reported in the paper: Eplerenone; Compound label in the paper: eplerenone

Published experiments with eplerenone; no Adooq supplier, lot, purity or formulation equivalence is established.

Reporter gene assays; Results: AZD9977 is a partial MR antagonist in vitro; Fig. 2a–b and caption

Inhibition of aldosterone-activated full-length human MR reporter: Luciferase reporter; Fig. 2 reports n = 4 and average ± SD for concentration-response curves. — Results paragraph immediately preceding Fig. 2; Fig. 2a and caption

MR reporter activation without aldosterone: Aldosterone-absent reporter condition; n = 4, average ± SD for plotted data. — Results paragraph immediately preceding Fig. 2; Fig. 2b and caption

In Vivo Studies

In male Wistar rats assessed four weeks after MI, dietary eplerenone at 100 mg/kg/day improved ventricular function compared with vehicle, while LVEF and filling pressure remained abnormal relative to sham controls. Changes in loading conditions may contribute to these functional effects. [2]

Post-MI cardiac responses depended on salt conditions in a separate rat experiment: eplerenone improved EF/FS and reduced fibrosis under high salt, while no significant functional benefit or observable antifibrotic effect was reported under low salt. The null findings do not establish equivalence. [3]

Partial improvement of post-infarction ventricular function

Animal study · Male Wistar rats after coronary-ligation myocardial infarction; sham-operated controls [2]

Dietary eplerenone improved LVEF and reduced LV end-diastolic pressure at four weeks, with values remaining abnormal relative to sham-operated rats.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Left ventricular ejection fraction at four weeksLVEF (%) Sham 64 (2); MI vehicle 31 (2); MI eplerenone 39 (2). Mean (SEM); n = 8, 9, 9 respectively. Eplerenone vs vehicle p < 0.05; both MI groups vs sham p < 0.01.[2]
Left ventricular end-diastolic pressure at four weeksLVEDP (mm Hg) Sham 3.7 (0.4); MI vehicle 14.8 (1.1); MI eplerenone 11.2 (0.6). Mean (SEM); n = 8, 9, 9 respectively. Eplerenone vs vehicle p < 0.01; both MI groups vs sham p < 0.01.[2]
Mean blood pressure and infarct-size controlsBetween-group comparison Mean blood pressure: no significant difference among groups. Infarct size: no significant difference between MI groups.[2]

Conditions shared by the study groups

Route
Oral, in food
Frequency
Daily dietary regimen
Treatment course
Assessment four weeks after MI
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Post-MI eplerenone
100 mg/kg/day		MI vehicle group; sham-operated group. Table 1/2 n = 9 eplerenone, 9 vehicle, 8 sham.LVEF increased and LVEDP decreased relative to MI vehicle, but neither returned to sham values.[2]
Post-MI eplerenone
Model: Male Wistar rats surviving overnight after MI; infarcts <30% excluded
Reported limits: Food formulation and actual individual intake/exposure are not specified in the read protocol.
Methods and source locations

Compound reported in the paper: Eplerenone; Compound label in the paper: eplerenone

Published experiments with eplerenone; no Adooq supplier, lot, purity or formulation equivalence is established.

Experimental animals and protocol; Doppler echocardiographic studies and physiological studies; Statistical analysis; Results; Tables 1–2 and footnotes; Discussion: body weight, diuresis and loading conditions

Left ventricular ejection fraction at four weeks: Blinded Doppler/2D echocardiographic assessment; modified Simpson method. — Table 2, LVEF row, Number row and footnotes; Doppler echocardiographic methods

Left ventricular end-diastolic pressure at four weeks: Physiological measurement; group comparisons by ANOVA and Student-Newman-Keuls test. — Table 1, LVEDP row, Number row and footnotes; Statistical analysis

Mean blood pressure and infarct-size controls: Control outcomes accompanying haemodynamic and ventricular assessment. — Results: Changes in haemodynamic variables and ventricular weights; Table 1

Post-MI eplerenone · Experimental animals and protocol; physiological methods; Tables 1–2

Salt-dependent post-infarction cardiac response

Animal study · Male Wistar rats with myocardial infarction assigned to normal-, low- or high-salt conditions, with eplerenone in low- and high-salt groups [3]

Eplerenone improved ventricular function and reduced cardiac fibrosis in the high-salt condition; no significant functional benefit or observable antifibrotic effect was reported in the low-salt condition.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
EF and fractional shortening at four weeksTreatment comparison High salt: significant improvement with eplerenone (p < 0.05 vs CH). Low salt: no significant eplerenone effect reported.[3]
Interstitial and perivascular myocardial fibrosisTreatment comparison High salt: both fibrosis measures reduced by eplerenone (Fig.5: interstitial p < 0.01, perivascular p < 0.05 vs CH). Low salt: no observable eplerenone effect reported.[3]

Conditions shared by the study groups

Route
Oral, in food
Frequency
Daily dietary regimen
Treatment course
4 weeks
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
EpH: eplerenone under high salt
100 mg/kg/day		CH: corresponding high-salt group without eplerenone.Improved EF/FS and lower interstitial/perivascular fibrosis relative to CH.[3]
EpL: eplerenone under low salt
100 mg/kg/day		CL: corresponding low-salt group without eplerenone.No significant improvement in EF/FS and no observable reduction in fibrosis versus CL were reported.[3]
EpH: eplerenone under high salt
Model: Post-MI male Wistar rats; 0.9% NaCl in drinking water
Reported limits: Group n and background chow composition for the high-salt condition are not specified in the read protocol.
EpL: eplerenone under low salt
Model: Post-MI male Wistar rats; 0.015% NaCl chow
Reported limits: Group n was not found in the acquired main paper; absence of significance does not establish equivalence.
Methods and source locations

Compound reported in the paper: Eplerenone; Compound label in the paper: eplerenone

Published experiments with eplerenone; no Adooq supplier, lot, purity or formulation equivalence is established.

PDF pp. 628–630 Methods/Results; p.632 Fig.5; p.633 Acknowledgements

EF and fractional shortening at four weeks: Echocardiography; mean ± SEM for plotted data; exact bar values not extracted. — p.630 Fig.2a–b/caption and Cardiac Function Results

Interstitial and perivascular myocardial fibrosis: Sirius-red collagen area relative to myocardial cross-sectional area; two blinded assessors; mean ± SEM. — pp.628–629 Histological Examination; pp.630–632 Cardiac Fibrosis Results; p.632 Fig.5a–b/caption

EpH: eplerenone under high salt · p.628 Experimental Protocol; p.630 Fig.2 and Results; p.632 Fig.5

EpL: eplerenone under low salt · p.628 Experimental Protocol; p.630 Cardiac Function and Cardiac Fibrosis Results; p.632 Fig.5

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 107724-20-9
Applications Aldosterone Blocker
Formula C24H30O6
Molecular Weight 414.49
Synonyms Epoxymexrenone
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

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Krister Bamberg, Ulrika Johansson, Karl Edman, et al. Preclinical pharmacology of AZD9977: A novel mineralocorticoid receptor modulator separating organ protection from effects on electrolyte excretion PLoS ONE (2018). PMID: 29474466 DOI: 10.1371/journal.pone.0193380 Source material
  2. [2] S Enomoto, M Yoshiyama, T Omura, et al. Effects of eplerenone on transcriptional factors and mRNA expression related to cardiac remodelling after myocardial infarction Heart (2005). PMID: 15797934 DOI: 10.1136/hrt.2004.046540 Source material
  3. [3] Akihiro Urabe, Takehiko Izumi, Yuichi Abe, et al. Effects of Eplerenone and Salt Intake on Left Ventricular Remodeling after Myocardial Infarction in Rats Hypertension Research (2006). PMID: 17137219 DOI: 10.1291/hypres.29.627 Source material

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