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Cyproterone acetate

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Chemical Structure| 427-51-0 同义名 : 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®
CAS号 : 427-51-0
货号 : A264009
分子式 : C23H27ClO4
纯度 : 98%
分子量 : 402.911
MDL号 : MFCD00864671
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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

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].
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 <<
实验方案
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
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