Apararenone

A non-steroidal mineralocorticoid receptor antagonist (Ki = 0.104 µM for the human receptor), selective for mineralocorticoid receptors over ERalpha and ERbeta and glucocorticoid, progesterone, and androgen receptors (IC50s = >100 µM for all), increases the urinary ratio of sodium to potassium in adrenalectomized rats, inhibits aldosterone- and nephrectomy-induced increases in systolic blood pressure and urinary albumin levels, as well as myocardial necrosis and fibrosis, cardiac arterial degeneration, and renal tubule damage, in a rat model of renal hypertension at 3 or 10 mg/kg per day. Formulation: A solid. InChI: InChI=1S/C17H17FN2O4S/c1-17(2)16(21)20(13-7-4-11(18)5-8-13)14-9-6-12(10-15(14)24-17)19-25(3,22)23/h4-10,19H,1-3H3. InChIKey: AZNHWXAFPBYFGH-UHFFFAOYSA-N. SMILES: CC1(C)OC2=CC(NS(C)(=O)=O)=CC=C2N(C3=CC=C(F)C=C3)C1=O