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: 427-51-0

Selleck's Cyproterone Acetate has been cited by 2 Publications

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Purity & Quality Control

Batch: Purity: 99.87%
99.87

Cyproterone Acetate Related Products

Signaling Pathway

Androgen Receptor Signaling Pathways

Androgen Receptor Signaling Pathway

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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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