Hubei Honest Biochemical Co., Ltd.

Eplerenone CAS 107724-20-9
Eplerenone

Product Name: Eplerenone

Synonyms: pregn-4-ene-7,21-dicarboxylic acid 9,11-epoxy-17-hydroxy-3-oxo gamma-lactone methyl ester;EPLERENONE 98%;EPLERENONE USP STANDARD;Elperenone;EplerenoneC24H3006;pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo, γ-lactone, methyl ester (7 α, 11 α, 17 α);EPLERENONE AND N-1 INTERMEDIATE;epoxymexrenone

CAS: 107724-20-9

MF: C24H30O6

MW: 414.49

Melting point 241-243°C

alpha D +5° (c = 0.437 in chloroform)

storage temp. Store at RT

solubility DMSO: soluble2mg/mL, clear (warmed)

Overview Eplerenone is in a class of medications called mineralocorticoid receptor antagonists. It can be used individually or in combination with other medications to treat hypertension by blocking the action of aldosterone, a natural substance in the body that raises blood pressure.

Chemical properties Eplerenone is an odorless, white to off-white crystalline powder. It is very slightly soluble in water, with its solubility essentially pH-independent. The octanol/water partition coefficient of eplerenone is approximately 7.1 at pH 7.0.

Mechanism of action Aldosterone,with many physiological and pathological effects, can cause central blood pressure and endothelial injury (catecholamines enhance its role), reduce heart rate variability, induce ventricular arrhythmias, and promote retention of sodium, potassium and magnesium loss, promote myocardial fibrosis, necrosis and inflammation, damage the fibrinolytic system.

Angiotensin converting enzyme inhibitors (also called angiotensin converting enzyme inhibitors, referred to as ACEI) and angiotensin Ⅱ receptor antagonist ARB aldosterone can inhibit the secretion of adrenaline, but after a period of treatment.The release of aldosterone was restored,which may even exceed the baseline plasma concentration levels. Despite adequate treatment of ACEI and ARB, aldosterone-induced damage can still happen, so it is necessary to use aldosterone receptor antagonists in the treatment of hypertension. Clinical studies have shown that patients who are not satisfied with the efficacy of ACEI or ARB therapy can add eplerenone along with the treatment.

Non-selective aldosterone receptor antagonist spironolactone can reduce mortality in patients with congestive heart failure, However, the side effects of male hyperplasia and other diseases associated with sex hormones have limited its application in the treatment of hypertension.