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Cyproterone acetate_分子结构_CAS_427-51-0)
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Cyproterone acetate

产品号 S2042 公司名称 Selleck Chemicals
CAS号 427-51-0 公司网站 http://www.selleckchem.com
分子式 C24H29ClO4 电 话 (877) 796-6397
分子量 416.93766 传 真 (832) 582-8590
纯 度 电子邮件 sales@selleckchem.com
保 存 -20°C Chembase数据库ID: 73284

产品价格信息

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产品别名

标题
Cyproterone acetate
IUPAC标准名
(1S,2S,3S,5R,11R,12S,15R,16S)-15-acetyl-9-chloro-2,16-dimethyl-6-oxopentacyclo[9.7.0.0^{2,8}.0^{3,5}.0^{12,16}]octadeca-7,9-dien-15-yl acetate
IUPAC传统名
cyproterone acetate

产品登记号

CAS号 427-51-0

产品性质

作用靶点 Estrogen receptor
成盐信息 acetate
保存条件 -20°C

产品详细信息

详细说明 (English)
Biological Activity
Description Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM.
Targets AR
IC50 7.1 nM [1]
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]
Clinical Trials Cyproterone acetate has entered in a phase III clinical trial in the treatment of anxiety disorder, prostate cancer, sexual dysfunction, urinary complications and long-term effects secondary to cancer therapy in adults.
Features
Combination Therapy
Description Cyproterone acetate plus bicalutamide, buserelin, flutamide, goserelin, leuprolide acetate and nilutamide has entered in a phase III clinical trial in the treatment of prostate cancer.
Protocol
Kinase Assay [1]
AR and ERα CALUX bioassays U2-OS cells are transfected with 3× HRE-TATA-Luc and pSG5-neo-hAR, using calcium phosphate precipitation to generate AR CALUX cells. AR and ERα CALUX cells are plated in 96-well plates (6000 cells/well) with phenol red-free DF medium supplemented with 5% dextran-coated charcoal-stripped FCS (DCC-FCS) at a volume of 200 μL per well. Two days later, the medium is refreshed, and cells are incubated with human or fetal serum (0–10% [v/v]) or Cyproterone acetate (dissolved in ethanol or DMSO) in triplicate at a 1:1000 dilution. In case of serum incubation, final serum concentration is 10% (v/v), and lower percentages of the tested sera are supplemented with DCC-FCS. After 24 hours the medium is removed, cells are lysed in 30 μL Triton-lysis buffer and measured for luciferase activity using a luminometer for 0.1 min/well.
Animal Study [2]
Animal Models Castrate male SD rat
Formulation Ethanol
Doses 0.2 mg /kg/day
Administration Administered via s.c.
References
[1] Sonneveld E, et al. Toxicol Sci. 2005, 83(1), 136-148.
[2] Attardi BJ, et al. Mol Cell Endocrinol. 2010, 328(1-2), 16-21.
[3] Arafa NM. Pak J Biol Sci. 2010, 13(20), 966-976.
[4] Santiago-Moreno J, et al. J Endocrinol. 2012.
[5] Aleem M, et al. Contraception. 2005, 71(5), 379-391.