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Eplerenone

Catalog No. T0083   CAS 107724-20-9
Synonyms: Epoxymexrenone, CGP 30083, SC-66110

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.

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Eplerenone Chemical Structure
Eplerenone, CAS 107724-20-9
Pack Size Availability Price/USD Quantity
5 mg In stock $ 44.00
10 mg In stock $ 63.00
25 mg In stock $ 127.00
50 mg In stock $ 193.00
100 mg In stock $ 273.00
500 mg In stock $ 677.00
1 g In stock $ 945.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.44%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Targets&IC50 Aldosterone:0.36 μM
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.
Synonyms Epoxymexrenone, CGP 30083, SC-66110
Molecular Weight 414.49
Formula C24H30O6
CAS No. 107724-20-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.1 mg/mL (10 mM)

TargetMolReferences and Literature

1. Kobayashi N, et al. Hypertension, 2005, 45(4), 538-544. 2. Keidar S, et al. J Cardiovasc Pharmacol, 2003, 41(6), 955-963. 3. Ward MR, et al. Circulation, 2001, 104(4), 467-472. 4. Suzuki G, et al. Circulation, 2002, 106(23), 2967-2972. 5. Lacolley P, et al. Circulation, 2002, 106(22), 2848-2853.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Glutamine Metabolism Compound Library Anti-Hypertension Compound Library Endocrinology-Hormone Compound Library Pediatric Drug Library Nuclear Receptor Compound Library

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Keywords

Eplerenone 107724-20-9 Endocrinology/Hormones Glucocorticoid Receptor Epoxymexrenone cardiovascular (CV) aldosterone atherosclerosis CGP-30083 CGP 30083 specific hypertension SC 66110 SC66110 inhibit Inhibitor CGP30083 Endogenous Metabolite SC-66110 MRA chronic systolic heart failure (HF) Mineralocorticoid Receptor inhibitor

 

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