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Submit ReviewEplerenone
Description: Selective mineralocorticoid receptor antagonist
Alternative Names: Inspra,Epoxymexrenone
Chemical Name: (7α,11α,17α)-9,11-Epoxy-17-hydroxy-3-oxo-pregn-4-ene-7,21-dicarboxylic acid γ-lactone methyl ester
Purity: ≥99% (HPLC)
Biological Activity for Eplerenone
Eplerenone is a selective mineralocorticoid (aldosterone) receptor antagonist (IC50 = 360 nM). Displays > 27-fold selectivity over androgen, progesterone and estrogen receptors (IC50 > 10 μM). Orally active antihypertensive in vivo.
Technical Data for Eplerenone
| M. Wt | 414.5 |
| Formula | C24H30O6 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 107724-20-9 |
| PubChem ID | 443872 |
| InChI Key | JUKPWJGBANNWMW-VWBFHTRKSA-N |
| Smiles | O=C1CC[C@@]2(C)C(C[C@@H]([C@](OC)=O)[C@]3([H])[C@@](O6)2[C@H]6C[C@@]4(C)[C@]([H])3CC[C@@]54OC(CC5)=O)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Eplerenone
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 4.14 | 10 |
Preparing Stock Solutions for Eplerenone
The following data is based on the product molecular weight 414.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 24.13 mL | 120.63 mL | 241.25 mL |
| 0.5 mM | 4.83 mL | 24.13 mL | 48.25 mL |
| 1 mM | 2.41 mL | 12.06 mL | 24.13 mL |
| 5 mM | 0.48 mL | 2.41 mL | 4.83 mL |
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Product Datasheets for Eplerenone
References for Eplerenone
References are publications that support the biological activity of the product.
De Gasparo et al (1987) Three new epoxy-spirolactone derivatives: characterization in vivo and in vitro. J.Pharmacol.Exp.Ther. 240 650 PMID: 2949071
McMahon and Cunningham (2001) Recent studies with eplerenone, a novel selective aldosterone receptor antagonist. Curr.Opin.Pharmacol. 1 190 PMID: 11714095
If you know of a relevant reference for Eplerenone, please let us know.
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Keywords: Eplerenone, Eplerenone supplier, Selective, mineralocorticoid, receptor, antagonists, Aldosterone, Receptors, Inspra, Epoxymexrenone, Mineralocorticoid, Receptor, 2397, Tocris Bioscience
2 Citations for Eplerenone
Citations are publications that use Tocris products. Selected citations for Eplerenone include:
Urbanet et al (2010) Analysis of Ins sensitivity in adipose tissue of patients with primary aldosteronism. Purinergic Signal 95 4037 PMID: 20484481
Ibrahim et al (2018) Mineralocorticoid Antagonist Improves Glucocorticoid Receptor Signaling and DEX Analgesia in an Animal Model of Low Back Pain. Front Cell Neurosci 12 453 PMID: 30524245
Do you know of a great paper that uses Eplerenone from Tocris? Please let us know.
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