A mineralocorticoid receptor antagonist
Related Products
Analytical Standard(s)
26302Eplerenone
Labeled Version(s)
31610Eplerenone-d3
Metabolite(s)
2802121-hydroxy Eplerenone 288596β-hydroxy Eplerenone
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Eplerenone

Item No. 15616

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(7α,11α,17α)-9,11-epoxy-17-hydroxy-3-oxo-pregn-4-ene-7,21-dicarboxylic acid, γ-lactone, 7-methyl ester
CAS Number
107724-20-9
Synonyms
  • CGP 30083
  • (+)-Eplerenone
  • Epoxymexrenone
  • SC-6110
  • SC-66110
Molecular Formula
C24H30O6
Formula Weight
414.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/ml
λmax
241 nm
SMILES
O=C1CC[C@@]2(C)C(C[C@@H](C(OC)=O)[C@]3([H])[C@]2(O4)[C@H]4C[C@@]5(C)[C@@]3([H])CC[C@]56OC(CC6)=O)=C1
InChi Code
InChI=1S/C24H30O6/c1-21-7-4-14(25)10-13(21)11-15(20(27)28-3)19-16-5-8-23(9-6-18(26)30-23)22(16,2)12-17-24(19,21)29-17/h10,15-17,19H,4-9,11-12H2,1-3H3/t15-,16+,17-,19+,21+,22+,23-,24-/m1/s1
InChi Key
JUKPWJGBANNWMW-VWBFHTRKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    Eplerenone is a mineralocorticoid receptor antagonist.1 It is selective for the mineralocorticoid receptor over glucocorticoid, androgen, progesterone, and estrogen receptors in radioligand binding assays (IC50s = 138, 6,920, 523, >10,000, and 5,702 nM, respectively). Eplerenone inhibits aldosterone-induced mineralocorticoid activity in a luciferase assay (IC50 = 122 nM). In vivo, eplerenone (100 mg/kg per day) reduces urinary albumin secretion and glomerulosclerosis in the Dahl salt-sensitive rat model of hypertension and nephropathy. It reduces myocardial IL-1β levels and collagen deposition, as well as improves left ventricular systolic dysfunction in a mouse model of acute myocardial infarction.2 Formulations containing eplerenone have been used in the treatment of hypertension and heart failure after myocardial infarction.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Meyers, M.J., Arhancet, G.B., Hockerman, S.L., et al. Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy. J. Med. Chem. 53(16), 5979-6002 (2010).

    2. Chen, B., Geng, J., Gao, S.-X., et al. Eplerenone modulates interleukin-33/sST2 signaling and IL-1β in left ventricular systolic dysfunction after acute myocardial infarction. J. Interferon. Cytokine Res. 38(3), 137-144 (2018).