产品说明书

Eplerenone

Print
Chemical Structure| 107724-20-9 同义名 : Epoxymexrenone;CGP 30083;Selara;Inspra;SC-6110;(+)-Eplerenone;SC-66110
CAS号 : 107724-20-9
货号 : A411181
分子式 : C24H30O6
纯度 : 98%
分子量 : 414.491
MDL号 : MFCD07783647
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(60.31 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Eplerenone is a potassium-sparing diuretic that selectively blocks aldosterone activation of the mineralcorticoid receptor (IC50 = 122 nM), demonstrating little activity towards other steroid receptors (IC50 > 9 µM for glucocorticoid, androgen, progesterone, and estrogen receptors), and is indicated for the treatment of hypertension and heart failure.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
293 cells Function assay 16 h Displacement of [3H]aldosterone from human mineralocorticoid receptor expressed in 293 cells after 16 hrs by scintillation counting, IC50=2.6 μM 25187277
COS1 cells Function assay 1 days Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay, IC50=1.3 μM 22074142
Huh7 cells Function assay Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay, IC50=0.122 μM 20672822
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.06mL

2.41mL

1.21mL

24.13mL

4.83mL

2.41mL
参考文献

[1]Kobayashi N, Hara K, et al. Eplerenone shows renoprotective effect by reducing LOX-1-mediated adhesion molecule, PKCepsilon-MAPK-p90RSK, and Rho-kinase pathway. Hypertension. 2005 Apr;45(4):538-44.

[2]Keidar S, Hayek T, et al. Effect of eplerenone, a selective aldosterone blocker, on blood pressure, serum and macrophage oxidative stress, and atherosclerosis in apolipoprotein E-deficient mice. J Cardiovasc Pharmacol. 2003 Jun;41(6):955-63.