product name Eplerenone
Description: Eplerenone (also known as CGP 30083, SC-66110) is a mineralocorticoid receptor antagonist, and blocks the action of aldosterone, used to control high blood pressure. Eplerenone inhibits upregulated phosphorylation of PKCepsilon, MAP kinase, and p90RSK in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone increases downregulated endothelial nitric oxide synthase mRNA in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone administration results in significant improvement in glomerulosclerosis and urinary protein in DS rats. Eplerenone (200 mg/kg/day) administration significantly decreases systolic and diastolic blood pressure by 12% and 11%, respectively, compared with untreated mice.
References: Hypertension. 2005 Apr;45(4):538-44; J Cardiovasc Pharmacol. 2003 Jun;41(6):955-63; Circulation. 2001 Jul 24;104(4):467-72.
414.49
Formula
C24H30O6
CAS No.
107724-20-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 4 mg/mL (9.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
CGP 30083, SC-66110
other peoduct :
| In Vitro |
In vitro activity: Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Eplerenone inhibits upregulated phosphorylation of PKCepsilon, MAP kinase, and p90RSK in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone increases downregulated endothelial nitric oxide synthase mRNA in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone administration results in significant improvement in glomerulosclerosis and urinary protein in DS rats. Eplerenone (200 mg/kg/day) administration significantly decreases systolic and diastolic blood pressure by 12% and 11%, respectively, compared with untreated mice. Eplerenone increases serum susceptibility to lipid peroxidation decreased by as much as 26%, and serum paraoxonase activity in mice. Eplerenone significantly reduces the atherosclerotic lesion area in aortas of mice, and this effect is reversed by AT-II. Eplerenone increases total vessel area by 30% and luminal area by nearly 60% compared with the no-treatment group, without affecting neointima size in pigs. Eplerenone significantly decreases LV end-diastolic wall stress in dogs. Eplerenone is associated with a 28% reduction in cardiomyocyte cross-sectional area, a 37% reduction of volume fraction of reactive interstitial fibrosis, and a 34% reduction of volume fraction of replacement fibrosis in dogs with heart failure. Eplerenone blunts the increase in pulse pressure in Aldo rats and normalized Einc-wall stress curves, medial cross-sectional area (MCSA), and EIIIA fibronectin in aldosterone (Aldo)-salt hypertensive rats. |
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| Formulation & Dosage | |
| References | Hypertension. 2005 Apr;45(4):538-44; J Cardiovasc Pharmacol. 2003 Jun;41(6):955-63; Circulation. 2001 Jul 24;104(4):467-72. |
