Cyproterone Acetate

Catalog No.S2042

Cyproterone Acetate Chemical Structure

Molecular Weight(MW): 416.94

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.

Size Price Stock Quantity  
In DMSO USD 50 In stock
USD 40 In stock
USD 90 In stock
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  • (C) Effect of AR antagonist cyproterone acetate (0–5 nM) on androgen-induced ADTRP transactivation in HeLa cells. (D) Effect of AR antagonist cyproterone acetate (0–0.5 nM) on androgen-induced ADTRP transactivation in HeLa cells

    Biochim Biophys Acta, 2017, 1863(9):2319-2332. Cyproterone Acetate purchased from Selleck.

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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

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 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]

Protocol

Animal Research:[2]
+ Expand
  • Animal Models: Castrate male SD rat
  • Formulation: Ethanol
  • Dosages: 0.2 mg /kg/day
  • Administration: Administered via s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL (199.06 mM)
Ethanol 10 mg/mL (23.98 mM)
Water Insoluble
In vivo Add solvents individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
20 mg/mL

* 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 416.94
Formula

C24H29ClO4

CAS No. 427-51-0
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03043924 Not yet recruiting Polycystic Ovary Syndrome University Hospital, Lille|National Research Agency, France March 2017 --
NCT02866786 Recruiting Polycystic Ovary Syndrome S.C.B. Medical College and Hospital August 2016 Phase 4
NCT02744131 Recruiting Polycystic Ovary Syndrome Kar Clinic & Hospital Pvt. Ltd.|All India Institute of Medical Sciences, New Delhi|Nova IVI Fertility, New Delhi|Dr Patils Fertility & Endoscopy Clinic, Bangalore|Shreyas Hospital & Sushrut Assisted Conception Clinic, Kolhapur May 2016 --
NCT02715232 Not yet recruiting Gender Dysphoria Medical University of Vienna May 2016 Phase 4
NCT02689843 Completed Polycystic Ovary Syndrome Shiraz University of Medical Sciences March 2016 Early Phase 1
NCT02410031 Completed Acne Vulgaris Bayer|RTI Health Solutions June 2015 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID