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环丙氯地孕酮

环丙氯地孕酮

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?环丙氯地孕酮名称


















中文名

环丙氯地孕酮
英文名

cyproterone acetate
中文别名


醋酸环丙孕酮




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醋酸环丙孕酮




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环丙孕酮醋酸盐




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6-氯-1α,2α-亚甲基-4,6-孕甾二烯-17α-羟基-3,20-二酮-17-醋酸酯




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奈非西坦



英文别名
更多





?环丙氯地孕酮生物活性












































描述
Cyproterone醋酸盐是高活性雄激素受体（AR）拮抗剂，IC50为7.1 nM，还是弱的孕酮受体激动剂。
相关类别



溶解度

体外：

H 2 O：<0.1 mg / mL（不溶）


储备液

1 mM 2.4819 mL 12.4097 mL 24.8194 mL
5 mM 0.4964 mL 2.4819 mL 4.9639 mL
10 mM 0.2482 mL 1.2410 mL 2.4819 mL


存储

粉末 -20℃下 3年
4℃下 2年
在溶剂中 -80℃下 6个月
-20℃下 1个月


运输

室温;可能会有所不同
SMILES

C[C@@]12C(C(Cl)=C[C@]3([H])[C@]2([H])C[C@@]4(C)[C@@]3([H])CC[C@]4(OC(C)=O)C(C)=O)=CC([C@H]5[C@@H]1C5)=O
参考文献

[1]. Sonneveld, E., 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. 83(1): p. 136-48.

[2]. Attardi, B.J., S. Koduri, and S.A. Hild, 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 End

[3]. Arafa, N.M., Efficacy of echinacea on the action of cyproterone acetate in male rats. Pak J Biol Sci, 2010. 13(20): p. 966-76.
相关活性
小分子



阿帕他胺



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去氢表雄酮



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氟他胺



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N-[(1S)-2-[3-(3-氯-4-氰基苯基)-1H-吡唑-1-基]-1-甲基乙基]-5-(1-羟基乙基)-1H-吡唑-3-甲酰胺



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达那唑



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3,3′-二吲哚甲烷



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AZD3514



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RAD140



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BMS-564929



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GLPG0492



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4-((R)-2-((R)-2,2,2-三氟-1-羟乙基)呲咯烷-1)-2-三氟甲基苯腈



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羽扇豆醇



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N-[4-硝基-3-(三氟甲基)苯基]-(2S)-3-[4-(乙酰基氨基)苯氧基]-2-羟基-2-甲基丙酰胺



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MK-0773



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ORM-15341






?环丙氯地孕酮物理化学性质














































密度 1.3±0.1 g/cm3
沸点 525.9±50.0 °C at 760 mmHg
熔点 200-201?C
分子式 C23H27ClO4
分子量 402.91
闪点 177.6±29.1 °C
PSA 60.44000
LogP 3.28
外观性状 气味
蒸汽压 0.0±1.4 mmHg at 25°C
折射率 1.582
储存条件 2-8°C
水溶解性 Practically insoluble in water, very soluble in methylene chloride, freely soluble in acetone, soluble in methanol, sparingly soluble in anhydrous ethanol.
计算化学

1.疏水参数计算参考值（XlogP）:3.6

2.氢键供体数量:0

3.氢键受体数量:4

4.可旋转化学键数量:3

5.互变异构体数量:10

6.拓扑分子极性表面积:60.4

7.重原子数量:29

8.表面电荷:0

9.复杂度:903

10.同位素原子数量:0

11.确定原子立构中心数量:8

12.不确定原子立构中心数量:0

13.确定化学键立构中心数量:0

14.不确定化学键立构中心数量:0

15.共价键单元数量:1





?环丙氯地孕酮毒性和生态




环丙氯地孕酮毒性英文版





?环丙氯地孕酮安全信息






































符号

GHS07

GHS08


GHS07, GHS08
信号词
Warning
危害声明
H312 + H332-H351
警示性声明
P261-P280
个人防护装备
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges
危害码 (欧洲)
Xn:Harmful
风险声明 (欧洲)
R20/21/22;R40
安全声明 (欧洲)
S26-S36
危险品运输编码 NONH for all modes of transport
WGK德国 3
RTECS号 GZ2230000
海关编码 2937290090











?环丙氯地孕酮海关









海关编码 2937290090








?环丙氯地孕酮文献69

更多文献














Estrogen and androgen regulate actin-remodeling and endocytosis-related genes during rat spermiation.

Mol. Cell. Endocrinol. 404 , 91-101, (2015)

Spermiation, the sperm release process, is imperative to male fertility and reproduction. Morphologically, it is characterized by removal of atypical adherens junctions called ectoplasmic specializati…



Effects of the anti-androgen cyproterone acetate (CPA) on oocyte meiotic maturation in rainbow trout (Oncorhynchus mykiss).

Aquat. Toxicol. 164 , 34-42, (2015)

In the present study, we aimed at characterizing the effect of cyproterone acetate (CPA), an anti-androgenic compound, on oocyte meiotic maturation in a freshwater teleost fish species, the rainbow tr…



Preservation of volumetric bone density and geometry in trans women during cross-sex hormonal therapy: a prospective observational study.

Osteoporos. Int. 26(1) , 35-47, (2015)

Although trans women before the start of hormonal therapy have a less bone and muscle mass compared with control men, their bone mass and geometry are preserved during the first 2?years of hormonal th…







?环丙氯地孕酮英文别名































































Cyprostat


(3aS,3bR,7aR,8aS,8bS,8cS,10aS)-1-Acetyl-5-chloro-8b,10a-dimethyl-7-oxo-1,2,3,3a,3b,7,7a,8,8a,8b,8c,9,10,10a-tetradecahydrocyclopenta[a]cyclopropa[g]phenanthren-1-yl acetate


Cyprosterone acetate


6-Chloro-1b,2b-dihydro-17-hydroxy-3′H-cyclopropa[1,2]pregna-1,4,6-triene-3,20-dione 17-Acetate


Pregna-4,6-diene-3,20-dione, 6-chloro-17-hydroxy-1α,2α-methylene-, acetate


Cyproterone 17-O-acetate


Cyproteron acetate


SH 714


(1R,3aS,3bR,7aR,8aS,8bS,8cS,10aS)-1-Acetyl-5-chloro-8b,10a-dimethyl-7-oxo-1,2,3,3a,3b,7,7a,8,8a,8b,8c,9,10,10a-tetradecahydrocyclopenta[a]cyclopropa[g]phenanthren-1-yl acetate


Cyproterone acetate


androcur


Cyproterone 17α-acetate


(1b,2b)-17-(Acetyloxy)-6-chloro-1,2-dihydro-3′H-cyclopropa[1,2]pregna-1,4,6-triene-3,20-dione


cPA


Cyproteron-R acetate


CpA (VAN)


Cyclopenta[a]cyclopropa[g]phenanthren-7(1H)-one, 1-acetyl-1-(acetyloxy)-5-chloro-2,3,3a,3b,7a,8,8a,8b,8c,9,10,10a-dodecahydro-8b,10a-dimethyl-, (1R,3aS,3bR,7aR,8aS,8bS,8cS,10aS)-


Cyproterone (acetate)








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