Cyproterone Acetate (Synonyms: CPA, Cyprostat, NSC 81430, SH 714) |
| رقم الكتالوجGC13971 |
سيبروتيرون أسيتات هو مضاد للأندروجين (IC50 = 7.1 نانومتر) وستيرويد صناعي بروجستيروني
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 427-51-0
Sample solution is provided at 25 µL, 10mM.
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.
| 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. | ||
| 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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)
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