Eplerenone

Eplerenone is a mineralocorticoid receptor antagonist. 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-1beta levels and collagen deposition, as well as improves left ventricular systolic dysfunction in a mouse model of acute myocardial infarction. Formulations containing eplerenone have been used in the treatment of hypertension and heart failure after myocardial infarction.Formal Name: (7alpha,11alpha,17alpha)-9,11-epoxy-17-hydroxy-3-oxo-pregn-4-ene-7,21-dicarboxylic acid, gamma-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: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml. lambdamax: 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.