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Cyproterone Acetate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cyproterone Acetate图片
CAS NO:427-51-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
250mg电议

产品介绍
Cyproterone acetate 是一种抗雄激素 (IC50=7.1 nM) 和孕激素合成类固醇。
Cas No.427-51-0
别名醋酸环丙孕酮
化学名(1aR,5aR,5bS,8R,8aS,10aS,10bS,10cS)-8-acetyl-4-chloro-8a,10b-dimethyl-2-oxo-1,1a,2,5a,5b,6,7,8,8a,9,10,10a,10b,10c-tetradecahydrocyclopenta[a]cyclopropa[g]phenanthren-8-yl acetate
Canonical SMILESClC1=C([H])C(C(C([H])([H])C2([H])[H])([H])C(C2(C(C([H])([H])[H])=O)OC(C([H])([H])[H])=O)(C([H])([H])[H])C([H])([H])C3([H])[H])([H])C3([H])C(C1=C([H])C4=O)(C([H])([H])[H])C5([H])C4([H])C5([H])[H]
分子式C24H29ClO4
分子量416.94
溶解度≥ 14.7mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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. Target: Androgen ReceptorCyproterone 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. 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].

References:
[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 Endocrinol, 2010. 328(1-2): p. 16-21.
[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.