الصفحة الرئيسية>>Signaling Pathways>> Endocrinology and Hormones>> Androgen Receptor>>Cyproterone Acetate

Cyproterone Acetate (Synonyms: CPA, Cyprostat, NSC 81430, SH 714)

رقم الكتالوجGC13971

سيبروتيرون أسيتات هو مضاد للأندروجين (IC50 = 7.1 نانومتر) وستيرويد صناعي بروجستيروني

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Cyproterone Acetate التركيب الكيميائي

Cas No.: 427-51-0

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
36٫00
متوفر
250mg
41٫00
متوفر

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مراجعات العميل

بناء على آراء العملاء.

Sample solution is provided at 25 µL, 10mM.

Description of Cyproterone Acetate

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.

Chemical Properties of Cyproterone Acetate

Cas No. 427-51-0 SDF
المرادفات CPA, Cyprostat, NSC 81430, SH 714
Chemical Name (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 SMILES ClC1=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]
Formula C24H29ClO4 M.Wt 416.94
الذوبان ≥ 14.7mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Cyproterone Acetate

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.3984 mL 11.9921 mL 23.9843 mL
5 mM 479.7 μL 2.3984 mL 4.7969 mL
10 mM 239.8 μL 1.1992 mL 2.3984 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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