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Purity: ≥98%
Eplerenone (also known as CGP 30083, Inspra, SC-66110) is a potent and selective mineralocorticoid receptor antagonist with an IC50 of 0.36 μM, it 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.
| ln Vitro |
With an IC50 value of 0.081 μM, eplerenone inhibits the human mineralocorticoid receptor[2].
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| ln Vivo |
In atherosclerotic apolipoprotein-deficient (EO) mice, eplerenone (200 mg/kg/day) orally for three months dramatically lowers oxidative stress and the progression of atherosclerosis [3].
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| Animal Protocol |
Animal/Disease Models: Atherosclerotic apolipoprotein Edeficient (EO) mice[3]
Doses: 200 mg/kg Route of Administration: po (oral gavage) 200 mg/kg/day for 3 months Experimental Results: Dramatically diminished systolic and diastolic blood pressure by 12% and 11%, respectively. diminished serum susceptibility to lipid peroxidation by as much as 26%, and increased serum paraoxonase activity by 28%. decreased levels of lipid peroxides, and Dramatically decreased macrophage oxidation of low-density lipoprotein (LDL) and superoxide ion release. Dramatically decreased the atherosclerotic lesion area. |
| References |
[1]. Myron H Weinberger, et al. Eplerenone, a selective aldosterone blocker, in mild-to-moderate hypertension. Am J Hypertens. 2002 Aug;15(8):709-16.
[2]. Dhillon, S., Eplerenone: a review of its use in patients with chronic systolic heart failure and mild symptoms. Drugs, 2013. 73(13): p. 1451-62. [3]. Shlomo Keidar, et al. Effect of eplerenone, a selective aldosterone blocker, on blood pressure, serum and macrophage oxidative stress, and atherosclerosis in apolipoprotein E-deficient mice. J Cardiovasc Pharmacol. 2003 Jun;41(6):955-63. |
| Molecular Formula |
C24H30O6
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| Molecular Weight |
414.49
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| CAS # |
107724-20-9
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| Related CAS # |
Eplerenone-d3
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| SMILES |
O1[C@]2([H])C([H])([H])[C@]3(C([H])([H])[H])[C@]4(C([H])([H])C([H])([H])C(=O)O4)C([H])([H])C([H])([H])[C@@]3([H])[C@]3([H])[C@]([H])(C(=O)OC([H])([H])[H])C([H])([H])C4=C([H])C(C([H])([H])C([H])([H])[C@]4(C([H])([H])[H])[C@]132)=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4126 mL | 12.0630 mL | 24.1260 mL | |
| 5 mM | 0.4825 mL | 2.4126 mL | 4.8252 mL | |
| 10 mM | 0.2413 mL | 1.2063 mL | 2.4126 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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