| Name | Eplerenone |
| Description | Eplerenone (CGP 30083) is an aldosterone receptor antagonist and potassium-sparing diuretic used in the therapy of hypertension. Eplerenone therapy has been associated with transient elevations in serum aminotransferase levels, but has yet to be linked to cases of clinically apparent drug induced liver disease. |
| In vitro | Eplerenone increases total vascular and luminal areas in swine without affecting the endothelial area. In canine models, it significantly reduces left ventricular end-diastolic wall stress. Eplerenone attenuates the rise in pulse pressure due to aldosterone (Aldo) in rats, normalizing the wall stress curve, mean cross-sectional area, and EIIIA fibronectin levels in Aldo-salt hypertensive rats. The compound upregulates diminished endothelial nitric oxide synthase mRNA in Dahl salt-sensitive hypertensive (DS) rats, markedly improving glomerulosclerosis and proteinuria. In mice, daily administration of 200 mg/kg of Eplerenone significantly lowers systolic and diastolic blood pressures compared to controls and increases serum phosphatase activity. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.41 mM), Sonication is recommended.
DMSO : 7.14 mg/mL (17.23 mM), Sonication is recommended.
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| Keywords | specific | SC66110 | SC 66110 | MRA | Mineralocorticoid Receptor | Inhibitor | inhibit | hypertension | GlucocorticoidReceptor | Glucocorticoid Receptor | Eplerenone | Endogenous Metabolite | chronic systolic heart failure (HF) | CGP-30083 | CGP30083 | cardiovascular (CV) | atherosclerosis | aldosterone |
| Inhibitors Related | Sucrose | Aceglutamide | Nicotinamide riboside malate | DL-Lysine | D(+)-Raffinose pentahydrate | Guanidine hydrochloride | Malic acid | Formamide | Glycerol | Thymidine | Corn starch | Gluconate Calcium |
| Related Compound Libraries | Nuclear Receptor Compound Library | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | Drug-induced Liver Injury (DILI) Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
