Catalog No.S4054

Spironolactone Chemical Structure

Molecular Weight(MW): 416.57

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

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In DMSO USD 90 In stock
USD 70 In stock
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1 Customer Review

  • (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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 416.57


CAS No. 52-01-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03314493 Completed Coronary Artery Calcification|Vascular Calcification Professor Fernando Figueira Integral Medicine Institute|Federal University of São Paulo November 7 2014 Phase 3
NCT01867294 Completed Advanced Malignant Neoplasm|Dermatologic Complication Academic and Community Cancer Research United|National Cancer Institute (NCI) August 31 2012 Phase 2
NCT02235077 Completed Heart Failure Duke University|National Heart Lung and Blood Institute (NHLBI) December 30 2014 Phase 2
NCT01712620 Recruiting Pulmonary Arterial Hypertension National Institutes of Health Clinical Center (CC)|National Heart Lung and Blood Institute (NHLBI)|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|University of Pennsylvania|University of Maryland|Washington Hospital Center|New England Medical Center Tufts University School of Medicine September 25 2012 Phase 1|Phase 2
NCT02901184 Recruiting Heart Failure With Preserved Ejection Fraction Uppsala University|Karolinska University November 23 2017 Phase 4
NCT03576755 Recruiting NASH - Nonalcoholic Steatohepatitis Monika Sarkar MD|University of California San Francisco October 2018 Phase 1|Phase 2

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Androgen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID