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/ Cyproterone acetate

醋酸环丙孕酮 /Cyproterone acetate {[allProObj[0].p_purity_real_show]}

货号：A264009 同义名： 醋酸环丙氯地孕酮 / Androcur;SH 714

Cyproterone Acetate is an antagonist and partial agonist of androgen receptor with IC50 value of 7.1 nM and EC50 value of 4μM.

Cyproterone acetate 化学结构 CAS号：427-51-0
Cyproterone acetate 化学结构
CAS号：427-51-0
Cyproterone acetate 3D分子结构
CAS号：427-51-0
Cyproterone acetate 化学结构 CAS号：427-51-0
Cyproterone acetate 3D分子结构 CAS号：427-51-0
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Cyproterone acetate 纯度/质量文件 产品仅供科研

货号：A264009 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Androgen Receptor ↓ 其他靶点 纯度
Cyproterone acetate ++++

Androgen Receptor, IC50: 7.1 nM

 		98%
Apalutamide +++

Androgen Receptor, IC50: 16 nM

 		98%
AZD3514 +

Androgen Receptor, Ki: 2.2 μM

 		98%
Darolutamide ++++

Androgen receptor, Ki: 11 nM

 		98%
Flutamide +++

Androgen Receptor, Ki: 55 nM

 		98%
Galeterone ++

Androgen Receptor, IC50: 384 nM

 		98%
Enzalutamide +++

Androgen Receptor, IC50: 36 nM

 		98%
Megestrol ✔ 98%
Bicalutamide ++

Androgen Receptor, IC50: 0.16 μM

 		99%
EPI-001 +

Androgen Receptor, IC50: ~6 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Cyproterone acetate 生物活性

靶点

  • Androgen Receptor

    Androgen Receptor, IC50:7.1 nM
描述 Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors. Cyproterone acetate is a partial agonist, showing agonism for the AR, with EC50 of 4.0 μM, at relatively high concentrations[3]. Cyproterone acetate but not AR antagonist bicalutamide dramatically increased the susceptibility of androgen receptor-negative human prostate cancer PC-3 and DU145 cells to TRAIL-induced apoptosis but no effects on immortalized human prostate stromal PS30 cells and human embryonic kidney HEK293 cells. Cyproterone acetate increases CHOP expression in a concentration and time-dependent manner and endoplasmic reticulum stress reducer 4-phenylbutyrate could block cyproterone acetate-induced CHOP (CCAAT-enhancer-binding protein homologous protein) and DR5 up-regulation[4]. Adult male C57 BL/6J mice injected with 0.08 mg/g of cyproterone acetate showed an increase in cellular lipid content in the zona fasciculata and zona retjculans of the adrenal cortex[5].

Cyproterone acetate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01550575 - Recruiting December 2022 United States, California ... 展开 >> Boston Scientific Clinical Research Information - Toll Free Number Recruiting Valencia, California, United States, 91355 Contact    855-213-9890    BSNClinicalTrials@bsci.com 收起 <<
NCT03630250 Meningitis, Bacterial ... 展开 >> Neisseria Infection 收起 << Early Phase 1 Recruiting September 1, 2020 United Kingdom ... 展开 >> NIHR Southampton Clinical Research Facility Recruiting Southampton, United Kingdom Contact       UHS.recruitmentCRF@nhs.net 收起 <<
NCT00401297 - Completed - Colombia ... 展开 >> Centro Internacional de Entrenamiento e Investigaciones Medicas, CIDEIM Cali, Colombia 收起 <<

Cyproterone acetate 参考文献

[1]Attardi BJ, Koduri S, et al. Relative progestational and androgenic activity of four progestins used for male hormonal contraception assessed in vitro in relation to their ability to suppress LH secretion in the castrate male rat. Mol Cell Endocrinol. 2010 Oct 26;328(1-2):16-21.

[2]Sonneveld E, Jansen HJ, et al. Development of androgen- and estrogen-responsive bioassays, members of a panel of human cell line-based highly selective steroid-responsive bioassays. Toxicol Sci. 2005 Jan;83(1):136-48.

[3]Sonneveld E, Jansen HJ, Riteco JA, Brouwer A, van der Burg B. Development of androgen- and estrogen-responsive bioassays, members of a panel of human cell line-based highly selective steroid-responsive bioassays. Toxicol Sci. 2005 Jan;83(1):136-48

[4]Chen L, Wolff DW, Xie Y, Lin MF, Tu Y. Cyproterone acetate enhances TRAIL-induced androgen-independent prostate cancer cell apoptosis via up-regulation of death receptor 5. BMC Cancer. 2017 Mar 7;17(1):179

[5]Migally N. Effect of cyproterone acetate on the structure of the adrenal cortex. Arch Androl. 1979 Mar;2(2):109-15

Cyproterone acetate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.48mL

0.50mL

0.25mL

12.41mL

2.48mL

1.24mL

24.82mL

4.96mL

2.48mL

Cyproterone acetate 技术信息

CAS号427-51-0
分子式C23H27ClO4
分子量 402.911
别名 醋酸环丙氯地孕酮 ;Androcur;SH 714;Androcur, Cyprostat,Cyproteron, Procur, Cyprone, Cyprohexal, Ciproterona, Cyproteronum, Neoproxil, Siterone.;NSC 81430;Cyprostat;CPA;Androcur®
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 35 mg/mL(86.87 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 20 mg/mL(49.64 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 27 mg/mL suspension

Tags: Cyproterone | 427-51-0 | Androgen Receptor | steroid | Androgen Receptor Antagonist | Vitamin D Related/Nuclear Receptor | Androgen Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Cyproterone acetate 纯度/质量文件 | Cyproterone acetate 亚型比较 | Cyproterone acetate 生物活性 | Cyproterone acetate 临床数据 | Cyproterone acetate 参考文献 | Cyproterone acetate 实验方案 | Cyproterone acetate 技术信息

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