Eplerenone (Synonyms: CGP 30083, (+)-Eplerenone, Epoxymexrenone, SC-6110, SC-66110) |
| Catalog No.GC15831 |
Eplerenone is an orally active mineralocorticoid receptor (MR) antagonist that blocks the effects of aldosterone, with an IC50 value of 0.081μM.
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Synonyms | CGP 30083, (+)-Eplerenone, Epoxymexrenone, SC-6110, SC-66110 | ||
| Chemical Name | (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] | ||
| Formula | C24H30O6 | M.Wt | 414.49 |
| Solubility | ≥ 4.6mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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