product name Cyproterone Acetate
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. It works by blocking androgen receptors which prevents androgens from binding to them and suppresses luteinizing hormone, which in turn reduces testosterone levels. It is primarily used to treat prostate cancer, benign prostatic hyperplasia, priapism, hypersexuality and other conditions.
References: Toxicol Sci. 2005 Jan;83(1):136-48; Mol Cell Endocrinol. 2010 Oct 26;328(1-2):16-21.
416.94
Formula
C24H29ClO4
CAS No.
427-51-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 83 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: 10 mg/mL (24.0 mM)
Solubility (In vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 20 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394970
| In Vitro |
In vitro activity: 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. 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. 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. Cyproterone acetate treatment plus artificial long days in autumn has a negative effect on sperm motility and sperm morphology. Androgen receptor occupation by Cyproterone acetate preferentially reduces the levels of spermatidal protamine in testis and spermatozoa involved in nuclear chromatin condensation. |
| Animal model | Castrate male SD rat |
| Formulation & Dosage | Dissolved in ethanol; 0.2 mg /kg/day; s.c administration |
| References | Toxicol Sci. 2005 Jan;83(1):136-48; Mol Cell Endocrinol. 2010 Oct 26;328(1-2):16-21. |
Related Posts
product name Cyproterone Acetate
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. It works by blocking androgen receptors which prevents androgens from binding to them and suppresses luteinizing hormone, which in turn reduces testosterone levels. It is primarily used to treat prostate cancer, benign prostatic hyperplasia, priapism, hypersexuality and other conditions.
References: Toxicol Sci. 2005 Jan;83(1):136-48; Mol Cell Endocrinol. 2010 Oct 26;328(1-2):16-21.
416.94
Formula
C24H29ClO4
CAS No.
427-51-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 83 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: 10 mg/mL (24.0 mM)
Solubility (In vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 20 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394970
| In Vitro |
In vitro activity: 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. 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. 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. Cyproterone acetate treatment plus artificial long days in autumn has a negative effect on sperm motility and sperm morphology. Androgen receptor occupation by Cyproterone acetate preferentially reduces the levels of spermatidal protamine in testis and spermatozoa involved in nuclear chromatin condensation. |
| Animal model | Castrate male SD rat |
| Formulation & Dosage | Dissolved in ethanol; 0.2 mg /kg/day; s.c administration |
| References | Toxicol Sci. 2005 Jan;83(1):136-48; Mol Cell Endocrinol. 2010 Oct 26;328(1-2):16-21. |