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Spironolactone Androgen Receptor antagonist

Cat.No.S4054

Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.
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Quality Control

Batch: Purity: 99.80%
99.80

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (199.24 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 27 mg/mL

Water : Insoluble

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In vivo
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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.
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Chemical Information, Storage & Stability

Molecular Weight 416.57 Formula

C24H32O4S

Storage (From the date of receipt)
CAS No. 52-01-7 Download SDF Storage of Stock Solutions

Synonyms N/A SMILES CC(=O)SC1CC2=CC(=O)CCC2(C3C1C4CCC5(C4(CC3)C)CCC(=O)O5)C

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Mechanism of Action

Targets/IC50/Ki
Androgen Receptor
77 nM
In vitro
Spironolactone is a strong AR antagonist (IC50 ~ 77 nM), a weak GR antagonist (IC50 ~ 2.4 μM), and a weak PR agonist (EC50 ~ 740 nM). This compound inhibits androstanolone binding in rat prostate nuclei and androstanolone specific binding in rat prostate cytosol.
In vivo
Spironolactone (1 mg/day) exerts anti-androgenic activity in rats. A single pretreatment of this compound (1 mg/rat) inhibits specific and saturable uptake of hormone into prostate induced by tracer dose administration of [3H]testosterone.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-06-13)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07020104 RECRUITING
Chronic Kidney Diseases
Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)
2025-01-07
NCT07645300 NOT_YET_RECRUITING
Hypertension Treated With Antihypertensive Drugs; Chronic Kidney Disease, 3B and 4
VA Office of Research and Development
2026-10-01 PHASE2
NCT07539259 NOT_YET_RECRUITING
Aortic Stenosis
University College, London
2026-12 PHASE2
NCT03984591 ENROLLING_BY_INVITATION
Systolic Heart Failure
Bispebjerg Hospital
2020-11-01 PHASE4
NCT07483177 RECRUITING
Thoracic Aortic Aneurysm
Mayo Clinic
2026-05-25 PHASE1; PHASE2
NCT07585526 NOT_YET_RECRUITING
MASLD; Chronic Kidney Diseases
Institute of Liver and Biliary Sciences, India
2026-04-15

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