Eplerenone-d3

Eplerenone-d₃ is intended for use as an internal standard for the quantification of eplerenone by GC- or LC-MS. 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.

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 nephropathyJ. 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 infarctionJ. Interferon. Cytokine Res.38(3)137-144(2018)