Eplerenone (97%)

• CAS: 107724-20-9
• Catalog Number: ALC-FP-107724209
• Category: Featured Products
• Molecular Weight: 414.5
• Molecular Formula: C24H30O6
• Melting Point: 220~225ºC
• Appearance: White Solid
• Sample Lot No.: A23M0916x2425
• Specific Rotation: (-)0.3° (c=1, CHCl13)

Case Study

Eplerenone Inhibits Macrophage-to-Myofibroblast Transition via MR/CTGF Pathway in UUO-Induced Cardiorenal Syndrome

Huan Y, et al. International Immunopharmacology, 2022, 113, 109396.

In a rat unilateral ureteral obstruction (UUO) model mimicking type 4 cardiorenal syndrome, eplerenone, a selective mineralocorticoid receptor (MR) antagonist, was employed to evaluate its antifibrotic effects. Histological analysis revealed severe fibrosis in both cardiac and renal tissues, accompanied by macrophage-to-myofibroblast transition (MMT). Administration of eplerenone effectively attenuated these fibrotic changes. In vitro, macrophages exposed to aldosterone exhibited MR activation, triggering MMT and upregulation of connective tissue growth factor (CTGF). Eplerenone treatment suppressed MR activation, reducing CTGF secretion and MMT induction. Furthermore, blockade of CTGF directly alleviated both aldosterone- and CTGF-driven MMT. These findings highlight the experimental application of eplerenone in modulating the MR/CTGF signaling cascade, thereby suppressing MMT-mediated fibrosis.

Comparative Clinical Outcomes of Eplerenone in Heart Failure Patients

Pardo-Martínez P, et al. European Journal of Internal Medicine, 2022, 97, 86-94.

In a real-world observational study, eplerenone was evaluated against spironolactone for its therapeutic impact in patients with heart failure and reduced ejection fraction (HFrEF). A total of 293 patients receiving eplerenone were propensity-score matched to 293 patients treated with spironolactone, selected from a prospective cohort of 1404 individuals managed in a specialized heart failure clinic. Fine-Gray competing risk regression was applied to analyze outcomes over a median follow-up of 3.95 years. The primary composite endpoint of cardiovascular death or hospitalization did not significantly differ between groups. However, eplerenone demonstrated superior effects, with significantly reduced cardiovascular mortality (HR 0.55) and all-cause mortality (HR 0.67). Importantly, discontinuation due to adverse events was less frequent with eplerenone. This study highlights the clinical application of eplerenone under rigorous real-world conditions, demonstrating its favorable safety and survival benefit compared to spironolactone in long-term management of HFrEF.

Eplerenone in Preventing Atrial Remodeling Induced by Chronic Intermittent Hypoxia

Yang Y, et al. Cardiovascular Pathology, 2022, 60, 107432.

A controlled rat study investigated the protective effects of eplerenone, a selective mineralocorticoid receptor antagonist, against atrial remodeling induced by chronic intermittent hypoxia (CIH). Ninety male Sprague-Dawley rats were assigned to control, CIH, and CIH-eplerenone (CIH-E) groups. The CIH model was maintained for six weeks, while the CIH-E group received daily oral gavage of eplerenone (10 mg/kg). Structural, molecular, and electrophysiological changes were systematically assessed using histopathology, JAK/STAT3 pathway analysis, isolated electrophysiology, and patch clamp recordings. CIH exposure caused atrial enlargement, fibrosis, reduced effective refractory period, and impaired ion channel function. Eplerenone intervention significantly mitigated these alterations by downregulating JAK/STAT3 signaling, restoring ion current density, and reducing atrial fibrillation inducibility.

Eplerenone Therapy in Bilateral Bullous Central Serous Chorioretinopathy: Clinical Evaluation

WJ, et al. American Journal of Ophthalmology Case Reports, 2022, 28, 01739.

A 30-year-old male with bilateral bullous central serous chorioretinopathy (bCSCR) was administered oral eplerenone as a mineralocorticoid receptor antagonist to reduce subretinal fluid. Despite continuous treatment, the left eye exhibited persistent fluid accumulation, while the right eye received adjunctive photodynamic therapy (PDT). Optical coherence tomography and fundus examination confirmed significant resolution of subfoveal subretinal fluid and restoration of visual acuity (20/200 → 20/25) post-PDT. Long-term follow-up (3.5 years) revealed stability without eplerenone, demonstrating limited efficacy of eplerenone monotherapy and highlighting PDT as a more effective therapeutic intervention in refractory bCSCR.