Home Endocrinology & Hormones Androgen Receptor antagonist Cyproterone Acetate For research use only.

Cyproterone Acetate

Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.

Cyproterone Acetate Chemical Structure

Cyproterone Acetate Chemical Structure

CAS No. 427-51-0

Purity & Quality Control

Cyproterone Acetate Related Products

Signaling Pathway

Androgen Receptor Signaling Pathways

Androgen Receptor Signaling Pathway

Biological Activity

Description Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.
Targets
Androgen Receptor [1]
7.1 nM
In vitro
In vitro Cyproterone acetate clearly shows antagonistic properties, while being a partial agonist also, showing agonism for the AR, with EC50 of 4.0 μM, at relatively high concentrations. [1] In the presence of 10 nM Testosterone, low concentrations of Cyproterone acetate inhibits T-stimulated transcription of 3XHRE-LUC, but at higher concentrations, transcription is stimulated. [2]
In Vivo
In vivo LH levels in Cyproterone acetate-treated rats do not dip below pretreatment levels, although they does not increase as much in the rats treated with 3.2 mg Cyproterone acetate/kg/day as in those which received 0.2 mg Cyproterone acetate/kg/day. [2] Cyproterone acetate exhibits direct negative effect on reproductive organs weight and significant reducing effect on sperm count and Ca2+ contents. SOD and GST activities significantly decrease in addition to significant increase in NO, MDA contents reflecting the oxidative status of testis in Cyproterone acetate treated rats. [3] Cyproterone acetate treatment plus artificial long days in autumn has a negative effect on sperm motility and sperm morphology. [4] Androgen receptor occupation by Cyproterone acetate preferentially reduces the levels of spermatidal protamine in testis and spermatozoa involved in nuclear chromatin condensation. [5]
Animal Research Animal Models Castrate male SD rat
Dosages 0.2 mg /kg/day
Administration Administered via s.c.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04925180 Completed
Signs of Androgenisation in Women e.g. Hirsutism Androgenetic Alopecia Acne and Seborrhea|Hypersexuality in Men|Sexual Deviations in Men|Prostate Cancer
Bayer
 October 18 2021 --
NCT02494297 Completed
Hirsutism|Androgenetic Alopecia|Severe Anemia|Seborrhea|PCOS
Center for Epidemiology and Health Research Germany|Bayer
 March 6 2015 --

Chemical Information & Solubility

Molecular Weight 416.94 Formula

C24H29ClO4
CAS No. 427-51-0 SDF Download Cyproterone Acetate SDF
Smiles CC(=O)C1(CCC2C1(CCC3C2C=C(C4=CC(=O)C5CC5C34C)Cl)C)OC(=O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 83 mg/mL ( (199.06 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble


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In vivo
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