Cyproterone Acetate

製品コードS2042 バッチS204203

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H29ClO4
分子量 416.94 CAS No. 427-51-0
Solubility (25°C)* 体外 DMSO 83 mg/mL (199.06 mM)
Ethanol 83 mg/mL (199.06 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
動物実験 動物モデル Castrate male SD rat
投薬量 0.2 mg /kg/day
投与方法 Administered via s.c.

カスタマーフィードバック

Data from [Data independently produced by , , Biochim Biophys Acta, 2017, 1863(9):2319-2332]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Cyproterone acetate acts as a disruptor of the aryl hydrocarbon receptor [ Sci Rep, 2021, 11(1):5457] PubMed: 33750846
Androgen inhibits key atherosclerotic processes by directly activating ADTRP transcription [Luo C, et al. Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332] PubMed: 28645652

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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