Cyproterone Acetate

製品コードS2042 バッチS204201

印刷

化学情報

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

10 mg/mL (23.98 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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は、IC50が7.1 nMのAndrogen Receptor（AR）アンタゴニストであり、弱いプロゲステロン受容体アゴニストであり、弱いプロゲスショナルおよびグルココルチコイド活性を持っています。
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. 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.
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.

プロトコル(参考用のみ)

キナーゼアッセイ	AR and ERα CALUX bioassays
キナーゼアッセイ	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.

参考

https://pubmed.ncbi.nlm.nih.gov/15483189/
https://pubmed.ncbi.nlm.nih.gov/20599585/
https://pubmed.ncbi.nlm.nih.gov/21319455/

https://pubmed.ncbi.nlm.nih.gov/22645301/
https://pubmed.ncbi.nlm.nih.gov/15854640/

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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：

Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271
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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。