Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5S-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
Purity: ≥98%
Formula Markup: C22H21F3N2O4S
Formula Weight: 466.5
CAS Number: 1632006-28-0
Notes: Esaxerenone is a non-steroidal mineralocorticoid receptor antagonist (IC50 = 9.4 nM).{68833} It is selective for mineralocorticoid receptors over glucocorticoid, androgen, and progesterone receptors (IC50s = >10,000 nM for all). Esaxerenone (0.3, 1, or 3 mg/kg) increases the urinary ratio of sodium to potassium in bilateral adrenalectomized rats. It decreases systolic blood pressure in DOCA-salt hypertensive rats when administered at a dose of 3 mg/kg to a greater extent than the mineralocorticoid receptor antagonists spironolactone or eplerenone (Item No. 15616). Esaxerenone (2 mg/kg per day) reduces systolic blood pressure, urinary protein levels, blood levels of brain natriuretic peptide (BNP), kidney and left ventricle weights, and glomerulosclerosis, as well as increases blood potassium levels, in Dahl salt-sensitive rats fed a high-salt diet.{68834} Formulations containing esaxerenone have been used in the treatment of hypertension.
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