GLPBio

Eplerenone

Catalog No.: GC15831Purity:>98.00%Synonyms: CGP 30083, (+)-Eplerenone, Epoxymexrenone, SC-6110, SC-66110
COASDSData Sheet
Eplerenon (Epoxymexrenon) ist ein selektiver, hochspezifischer und oral aktiver Aldosteronblocker (SAB).

Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.

Eplerenone
Cas No.: 107724-20-9
10mM (in 1mL DMSO)In Stock
$38.00
1
10mgIn Stock
$52.00
1
25mgIn Stock
$91.00
1
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Beschreibung (Description)

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.

Protokoll (Protocol)

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:
[1]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.
[2]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.

Produktdokumente (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
107724-20-9
Synonyme
CGP 30083, (+)-Eplerenone, Epoxymexrenone, SC-6110, SC-66110
Chemischer 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
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]
Summenformel
C24H30O6
Molekulargewicht
414.49
Löslichkeit
≥ 4.6mg/mL in DMSO with gentle warming
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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