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Catalog No.S4054

8 publications

Spironolactone Chemical Structure

CAS No. 52-01-7

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

Selleck's Spironolactone has been cited by 8 publications

2 Customer Reviews

  • (h and i) Triptolide inhibits transcription. After exposure to triptolide (1 μm), spironolactone (10 μm), actinomycin D (2 μm, transcription inhibitor used as a positive control) or DMSO for 6 h, the global RNA synthesis was evaluated by the measurement of 5-EU incorporation. The figure shows representative merged pictures of DAPI and 5-EU signal. The intensity of the signal was evaluated through fluorescence microscopy (h) and quantified with the CellProfiler Software. Triptolide but not spironolactone inhibits global transcription.

    Leukemia, 2018, 32(1):111-119. Spironolactone purchased from Selleck.

    (A, B) Indicated HIV-1 latency cells (A. J-LAT 10.6; B. CA5) were treated with levosimendan or spironolactone (5, 10, or 20 μM) in combination with TNFα (10 ng/ml). After 24 hr, mRNA was extracted, and reverse transcribed to cDNA for measurement of HIV-1 initiated or elongated (proximal [Pro], intermediate [Int], and distal [Dis]) transcripts by qPCR. Results were normalized to DMSO control. Values represent the mean ± s.d. (n = 4-6).

    Antiviral Res, 2017, 146:76-85. Spironolactone purchased from Selleck.

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Biological Activity

Description Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.
Androgen Receptor [1]
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). [1] Spironolactone inhibits androstanolone binding in rat prostate nuclei and androstanolone specific binding in rat prostate cytosol. [2]

In vivo Spironolactone (1 mg/day) exerts anti-androgenic activity in rats. A single pretreatment of spironolactone (1 mg/rat) inhibits specific and saturable uptake of hormone into prostate induced by tracer dose administration of [3H]testosterone. [2]


Solubility (25°C)

In vitro DMSO 83 mg/mL (199.24 mM)
Ethanol 20 mg/mL (48.01 mM)
Water Insoluble

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Chemical Information

Molecular Weight 416.57


CAS No. 52-01-7
Storage powder
in solvent
Synonyms N/A
Smiles CC(=O)SC1CC2=CC(=O)CCC2(C3C1C4CCC5(C4(CC3)C)CCC(=O)O5)C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04723862 Recruiting Drug: Spironolactone|Drug: Placebo Hyperandrogenism|Polycystic Ovary Syndrome|Puberty University of Virginia|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) February 1 2021 Early Phase 1
NCT03921476 Withdrawn Other: Online survey Acne Vulgaris Northwestern University July 1 2020 --
NCT03929718 Recruiting Drug: Spironolactone|Drug: No Spironolactone AFib Piedmont Healthcare April 24 2019 Early Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID