Eplerenone
(Synonyms: 依普利酮; Epoxymexrenone) 目录号 : GC15831
Eplerenone（依普利酮）是一种具有口服活性的盐皮质激素受体（MR）拮抗剂，它的作用是阻断醛固酮的作用，IC50值为0.081μM。
Cas No.:107724-20-9
Sample solution is provided at 25 µL, 10mM.
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Eplerenone is an orally active mineralocorticoid receptor (MR) antagonist that blocks the effects of aldosterone, with an IC50 value of 0.081μM[1, 2]. Eplerenone can be used in the study of hypertension, atherosclerosis, chronic systolic heart failure and cardiovascular diseases[3].
In vitro, Eplerenone (1µM) treatment of cardiomyocytes and fibroblasts for 24-48h promoted cardiomyocyte proliferation and increased cGMP activity[4]. Eplerenone (2µM) treatment of primary cultures of venous endothelial cells (EAHy 926) and human coronary artery endothelial cells (HCAEC) reversed aldosterone-induced endothelial cell growth and sclerosis in vitro[5].
In vivo, oral administration of Eplerenone (50mg/kg) to rats after unilateral ureteral obstruction (UUO) surgery inhibited the development of renal fibrosis, inflammation (macrophage and monocyte infiltration), interstitial cell proliferation and interstitial cell activation (α-SMA expression), and reduced oxidative stress[6]. Subcutaneous administration of Eplerenone (30mg/kg) to rats after unilateral hindlimb ischemia surgery significantly increased the number, colony formation and migration of endothelial progenitor cells (EPCs) after hindlimb ischemia, and decreased the expression of NAD(P)H oxidase p22 phox, p47 phox, gp91 phox and the expression of serum and glucocorticoid-induced aldosterone responsive kinase 1 (Sgk1)[7].
References:
[1] Coleman C I, Song J C, White C M. Eplerenone[J]. Formulary, 2002, 37(10): 514.
[2] Dhillon S. Eplerenone: a review of its use in patients with chronic systolic heart failure and mild symptoms[J]. Drugs, 2013, 73: 1451-1462.
[3] Funder J W. Eplerenone: hypertension, heart failure and the importance of mineralocorticoid receptor blockade[J]. Future Cardiology, 2006, 2(5): 535-541.
[4] Hermidorff M M, Faria G O, Amâncio G C S, et al. Non-genomic effects of spironolactone and eplerenone in cardiomyocytes of neonatal Wistar rats: do they evoke cardioprotective pathways?[J]. Biochemistry and Cell Biology, 2015, 93(1): 83-93.
[5] Hillebrand U, Schillers H, Riethmüller C, et al. Dose-dependent endothelial cell growth and stiffening by aldosterone: endothelial protection by eplerenone[J]. Journal of hypertension, 2007, 25(3): 639-647.
[6] Chen H, Sun F, Zhong X, et al. Eplerenone-mediated aldosterone blockade prevents renal fibrosis by reducing renal inflammation, interstitial cell proliferation and oxidative stress[J]. Kidney and Blood Pressure Research, 2013, 37(6): 557-566.
[7] Kobayashi N, Fukushima H, Takeshima H, et al. Effect of eplerenone on endothelial progenitor cells and oxidative stress in ischemic hindlimb[J]. American journal of hypertension, 2010, 23(9): 1007-1013.
| Cell experiment [1]: | |
Cell lines | Cardiomyocytes and fibroblasts |
Preparation Method | After preparing the cardiomyocyte and fibroblast cultures, both were incubated in a 37°C 5% CO2 incubator for approximately 36h to allow the cells to fully adhere. 104 cells were seeded per well in a 96-well plate and analyzed after treatment with spironolactone (1µM), Eplerenone (1µM), and mifepristone (10µM) for 0, 24, and 48h. In all assays, aldosterone (Sigma-Aldrich) was added to the cell culture medium for 10min only on the day of the assay. |
Reaction Conditions | 1µM; 24, 48h |
Applications | Both spironolactone and Eplerenone were able to promote cardiomyocyte proliferation in the absence and presence of aldosterone and to increase cGMP levels. |
| Animal experiment [2]: | |
Animal models | Wistar rats |
Preparation Method | Eplerenone or vehicle was given to male Wistar rats (50mg/kg, twice daily) for 7 days before unilateral ureteral obstruction (UUO) and for an additional 28 days after surgery. Body weight, blood pressure, renal histo-morphology, immune-staining for macrophages, monocyte chemotactic protein-1, proliferating cell nuclear antigen, α-smooth muscle actin, and serum and urine markers of renal function and oxidative stress were determined for both groups on 7, 14, and 28 days after surgery. |
Dosage form | 50mg/kg; p.o. |
Applications | Eplerenone inhibited the development of renal fibrosis, inflammation (macrophage and monocyte infiltration), interstitial cell proliferation, and activation of interstitial cells (α-SMA expression). Epleronone also reduced oxidative stress. |
References: | |
| Cas No. | 107724-20-9 | SDF | |
| 别名 | 依普利酮; Epoxymexrenone | ||
| 化学名 | (2'R,6R,6aR,6bS,9aS,10aR,11aR,11bS)-methyl 9a,11b-dimethyl-3,5'-dioxo-2,3,4',5,5',6,6a,6b,7,8,9a,10,10a,11b-tetradecahydro-1H,3'H-spiro[cyclopenta[1,2]phenanthro[4,4a-b]oxirene-9,2'-furan]-6-carboxylate | ||
| Canonical SMILES | O=C(C(C1([H])[H])([H])C2([H])C3(C(C([H])([H])C4([H])[H])(C([H])([H])[H])C1=C([H])C4=O)OC3([H])C([H])([H])C5(C([H])([H])[H])C2([H])C([H])([H])C([H])([H])[C@@]5(C([H])([H])C6([H])[H])OC6=O)OC([H])([H])[H] | ||
| 分子式 | C24H30O6 | 分子量 | 414.49 |
| 溶解度 | ≥ 4.6mg/mL in DMSO with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4126 mL | 12.063 mL | 24.126 mL |
| 5 mM | 0.4825 mL | 2.4126 mL | 4.8252 mL |
| 10 mM | 0.2413 mL | 1.2063 mL | 2.4126 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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