A mineralocorticoid receptor antagonist; selective for the mineralocorticoid receptor over glucocorticoid

Eplerenone – 25 mg

Brand:
Cayman
CAS:
107724-20-9
Storage:
-20
UN-No:
Non-Hazardous - /

Eplerenone is a mineralocorticoid receptor antagonist.{18724} 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.{59183} Formulations containing eplerenone have been used in the treatment of hypertension and heart failure after myocardial infarction.  

 

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Description

A mineralocorticoid receptor antagonist; 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); inhibits aldosterone-induced mineralocorticoid activity in a luciferase assay (IC50 = 122 nM); reduces urinary albumin secretion and glomerulosclerosis in the Dahl salt-sensitive rat model of hypertension and nephropathy at 100 mg/kg per day; reduces myocardial IL-1β levels and collagen deposition, as well as improves left ventricular systolic dysfunction in a mouse model of acute myocardial infarction

Formal name: (7α,11α,17α)-9,11-epoxy-17-hydroxy-3-oxo-pregn-4-ene-7,21-dicarboxylic acid, γ-lactone, 7-methyl ester

Synonyms:  (+)-Eplerenone|CGP 30083|Epoxymexrenone|SC-6110|SC-66110

Molecular weight: 414.5

CAS: 107724-20-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Cardiovascular Diseases|Myocardial Infarction||Research Area|Cardiovascular System|Heart||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Glucocorticoids & Mineralocorticoids

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