Eplerenone

SKU: orb1310957

Description

Eplerenone (CGP 30083) is a selective aldosterone antagonist used as an antihypertensive and cardioprotective agent. It is widely applied in cardiovascular research, including in vitro receptor binding assays and in vivo models of hypertension and heart failure.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 107724-20-9
• MW: 414.4914
• Purity: 99.84% (May vary between batches)
• Formula: C₂₄H₃₀O₆
• SMILES: COC(=O)[C@@H]1CC2=CC(=O)CC[C@]2(C)[C@@]23O[C@@H]2C[C@@]2(C)[C@@H](CC[C@@]22CCC(=O)O2)C13
• Target: Endogenous Metabolite,Glucocorticoid Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.41 mM);DMSO:7.14 mg/mL (17.23 mM)

Bioactivity

• Target IC50:
  Aldosterone:0.36 μM
• In Vitro:
  Eplerenone increases total vascular and luminal areas in swine without affecting the endothelial area. In canine models, it significantly reduces left ventricular end-diastolic wall stress. Eplerenone attenuates the rise in pulse pressure due to aldosterone (Aldo) in rats, normalizing the wall stress curve, mean cross-sectional area, and EIIIA fibronectin levels in Aldo-salt hypertensive rats. The compound upregulates diminished endothelial nitric oxide synthase mRNA in Dahl salt-sensitive hypertensive (DS) rats, markedly improving glomerulosclerosis and proteinuria. In mice, daily administration of 200 mg/kg of Eplerenone significantly lowers systolic and diastolic blood pressures compared to controls and increases serum phosphatase activity.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

aldosterone, cardiovascular (CV), atherosclerosis, CGP 30083, CGP30083, CGP-30083, chronic systolic heart failure (HF), Endogenous Metabolite, Inhibitor, hypertension, Glucocorticoid Receptor, GlucocorticoidReceptor, Eplerenone, Epoxymexrenone, Mineralocorticoid Receptor, MRA, inhibit, specific, SC 66110, SC66110, SC-66110

Compound Identifiers

PubChem CID

443872