产品描述:
Eplerenone-d3 is intended for use as an internal standard for the quantification of eplerenone (Item No. 15616) by GC- or LC-MS. 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.