货号:A411181 同义名: Epoxymexrenone;CGP 30083
Eplerenone is both a selective aldosterone blocker and a CYP3A4 substrate.
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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 |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 107724-20-9 |
分子式 | C24H30O6 |
分子量 | 414.491 |
别名 | Epoxymexrenone;CGP 30083;Selara;Inspra;SC-6110;(+)-Eplerenone;SC-66110 |
运输 | 蓝冰 |
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 |