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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.
Spironolactone Androgen Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 416.57

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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

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 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06021860 Not yet recruiting
Edema Due to Heart Failure or Cirrhosis
CMP Development LLC
June 2024 Phase 4
NCT06204640 Not yet recruiting
Atrial Fibrillation Recurrent
University Hospital Caen
March 1 2024 Phase 3
NCT05807139 Recruiting
Alcohol Use Disorder
National Institute on Drug Abuse (NIDA)|National Institutes of Health Clinical Center (CC)
July 13 2023 Phase 1
NCT05092984 Recruiting
Rheumatoid Arthritis
University Hospital Strasbourg France
June 22 2022 Phase 3
NCT04723862 Recruiting
Hyperandrogenism|Polycystic Ovary Syndrome|Puberty
University of Virginia|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)
November 12 2021 Early Phase 1

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