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Eplerenone Mineralocorticoid Receptor antagonist

Name: Eplerenone
SKU: S1707
Availability: InStock
Rating: 5 (6 reviews)

Cat.No.S1707

Eplerenone is a mineralocorticoid receptor antagonist, and blocks the action of aldosterone, used to control high blood pressure.

Chemical Structure

Molecular Weight: 414.49

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Opioid Receptor THR PGES Aromatase 5-alpha Reductase CCK receptor GHSR SSTR TSH Receptor GNRH Receptor PGDS
Related Products	Apararenone Canrenone Esaxerenone (CS-3150)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
Huh7 cells	Function assay		Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay, IC50=0.122 μM
COS1 cells	Function assay	1 days	Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay, IC50=1.3 μM
293 cells	Function assay	16 h	Displacement of [3H]aldosterone from human mineralocorticoid receptor expressed in 293 cells after 16 hrs by scintillation counting, IC50=2.6 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	414.49	Formula	C₂₄H₃₀O₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	107724-20-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CGP 30083, SC-66110			Smiles	CC12CCC(=O)C=C1CC(C3C24C(O4)CC5(C3CCC56CCC(=O)O6)C)C(=O)OC

Solubility

In vitro
Batch:

DMSO : 10 mg/mL (24.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5% 4-Methylpyridine 1 95%Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (12.06mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear 4-Methylpyridine stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.300mg/ml (0.72mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.300mg/ml (0.72mM)

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	mineralocorticoid receptor ^[1]
In vivo	Eplerenone inhibits upregulated phosphorylation of PKCepsilon, MAP kinase, and p90RSK in Dahl salt-sensitive hypertensive (DS) rats. This compound increases downregulated endothelial nitric oxide synthase mRNA in Dahl salt-sensitive hypertensive (DS) rats. Its administration results in significant improvement in glomerulosclerosis and urinary protein in DS rats. ^[1] This compound (200 mg/kg/day) administration significantly decreases systolic and diastolic blood pressure by 12% and 11%, respectively, compared with untreated mice. It increases serum susceptibility to lipid peroxidation decreased by as much as 26%, and serum paraoxonase activity in mice. This chemical significantly reduces the atherosclerotic lesion area in aortas of mice, and this effect is reversed by AT-II. ^[2] It increases total vessel area by 30% and luminal area by nearly 60% compared with the no-treatment group, without affecting neointima size in pigs. ^[3] This compound significantly decreases LV end-diastolic wall stress in dogs. It 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. ^[4] This chemical 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. ^[5]
References	[1] https://pubmed.ncbi.nlm.nih.gov/15710785/ [2] https://pubmed.ncbi.nlm.nih.gov/12775976/ [3] https://pubmed.ncbi.nlm.nih.gov/11468211/ [4] https://pubmed.ncbi.nlm.nih.gov/12460880/ [5] https://pubmed.ncbi.nlm.nih.gov/12451013/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06168994	Not yet recruiting	Paroxysmal Atrial Fibrillation	Assiut University	February 1 2024	Phase 4
NCT06208072	Recruiting	Primary Hypertension\|Obesity	Hippocration General Hospital\|National and Kapodistrian University of Athens	September 1 2023	Not Applicable

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