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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
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)416.94
FormulaC24H29ClO4
CAS No.427-51-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 83 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: 10 mg/mL (24.0 mM)
Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 20 mg/mL
Other info

Synonyms: Cyprone, Cyprohexal, Ciproterona, Cyproteronum, Androcur, Cyprostat,Cyproteron, Procur, Neoproxil, Siterone.

Chemical Name: (2aR,3aS,3bS,3cS,5aS,6R,8aS,8bR)-6-acetyl-10-chloro-3b,5a-dimethyl-2-oxo-2,2a,3,3a,3b,3c,4,5,5a,6,7,8,8a,8b-tetradecahydrocyclopenta[a]cyclopropa[g]phenanthren-6-yl acetate

InChi Key: UWFYSQMTEOIJJG-FDTZYFLXSA-N

InChi Code: InChI=1S/C24H29ClO4/c1-12(26)24(29-13(2)27)8-6-16-14-10-20(25)19-11-21(28)15-9-18(15)23(19,4)17(14)5-7-22(16,24)3/h10-11,14-18H,5-9H2,1-4H3/t14-,15+,16-,17-,18-,22-,23-,24-/m0/s1

SMILES Code: CC(O[C@]1(C(C)=O)CC[C@]2([H])[C@]1(C)CC[C@]3([H])[C@@]4(C)[C@](C5)([H])[C@]5([H])C(C=C4C(Cl)=C[C@@]23[H])=O)=O

实验参考方法
In Vitro

In vitro activity: 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 VivoLH 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.
Animal modelCastrate male SD rat
Formulation & DosageDissolved in ethanol; 0.2 mg /kg/day; s.c administration
References

Toxicol Sci. 2005 Jan;83(1):136-48; Mol Cell Endocrinol. 2010 Oct 26;328(1-2):16-21.