Eplerenone 是一种竞争性的、选择性的、具有口服活性的醛固酮 (aldosterone) 拮抗剂，IC50=138 nM。它对孕酮，雄激素，雌激素和糖皮质激素受体的亲和力低，可用于研究高血压和心肌梗死后的心力衰竭。

Eplerenone is an aldosterone receptor antagonist and potassium-sparing diuretic used in the therapy of hypertension. Eplerenone therapy has been associated with transient elevations in serum aminotransferase levels, but has yet to be linked to cases of clinically apparent drug induced liver disease.

Eplerenone在猪体内可以增加总血管面积和管腔面积,而不影响血管内膜的面积.在狗体内,其明显减少LV心脏舒张末期心室壁压力.Eplerenone减弱Aldo大鼠体内脉压的增加,并使醛固酮(Aldo)-盐高血压大鼠体内Einc壁压力曲线,平均横截面积和EIIIA纤连蛋白标准化.Eplerenone提高Dahl 盐敏感性高血压(DS)大鼠体内下调的内皮细胞一氧化氮合成酶mRNA,还明显改善了DS大鼠的肾小球硬化症和尿蛋白.与对照组小鼠相比,每天给药200 mg/kg Eplerenone明显降低心脏收缩压和舒张压.Eplerenone在小鼠体内,增加了血清对氧磷酶的活性.

107724-20-9

C24H30O6

414.49

CGP 30083;依普利酮;SC-66110;Epoxymexrenone

DMSO:4.1 mg/mL (10 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years