For research use only. Not for therapeutic Use.
Cyproterone acetate (Cat No.: I003528) is an androgen receptor antagonist, with an IC50 of 7.1 nM. It is also a weak progesterone receptor agonist with weak progesterone and glucocorticoid activities. Cyproterone acetate has significant antagonistic properties and also has some activator properties. When the concentration is relatively high, it activates AR, EC50 is 4.0 μ M. Chemicalbook In the presence of 10nM testosterone, low concentrations of Cyproteroneacetate inhibit T-stimulated 3XHRE-LUC transcription, but high concentrations stimulate transcription. It is clinically used to treat male benign prostatic hypertrophy and can be used as a male contraceptive.
| Catalog Number | I003528 |
| CAS Number | 427-51-0 |
| Synonyms | (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 |
| Molecular Formula | C24H29ClO4 |
| Purity | ≥95% |
| Target | Androgen Receptor |
| Solubility | DMSO 80 mg/mL; Water <1 mg/mL |
| Storage | 3 years -20C powder |
| InChIKey | UWFYSQMTEOIJJG-FDTZYFLXSA-N |
| Reference | </br>1:Consecutive Cyproterone Acetate and Estradiol Treatment in Late-Pubertal Transgender Female Adolescents. Tack LJW, Heyse R, Craen M, Dhondt K, Bossche HV, Laridaen J, Cools M.J Sex Med. 2017 May;14(5):747-757. doi: 10.1016/j.jsxm.2017.03.251. PMID: 28499525 </br>2:Use of cyproterone acetate/ethinylestradiol in polycystic ovary syndrome: rationale and practical aspects. Ruan X, Kubba A, Aguilar A, Mueck AO.Eur J Contracept Reprod Health Care. 2017 May 2:1-8. doi: 10.1080/13625187.2017.1317735. [Epub ahead of print] PMID: 28463030 </br>3:The use of cyproterone acetate/ethinyl estradiol in hyperandrogenic skin symptoms – a review. Bitzer J, Römer T, Lopes da Silva Filho A.Eur J Contracept Reprod Health Care. 2017 Apr 27:1-10. doi: 10.1080/13625187.2017.1317339. [Epub ahead of print] PMID: 28447864 </br>4:Prescription Appropriateness of Cyproterone Acetate/Ethinylestradiol in Primary Care: A Population-Based Study in Italy. Lapi F, Simonetti M, Cricelli I, Cricelli C, Cassano N, Vena GA.Clin Drug Investig. 2017 Apr 22. doi: 10.1007/s40261-017-0529-9. [Epub ahead of print] PMID: 28434141 </br>5:Cyproterone acetate enhances TRAIL-induced androgen-independent prostate cancer cell apoptosis via up-regulation of death receptor 5. Chen L, Wolff DW, Xie Y, Lin MF, Tu Y.BMC Cancer. 2017 Mar 7;17(1):179. doi: 10.1186/s12885-017-3153-4. PMID: 28270124 Free PMC Article</br>6:Response to /Letter to the Editor Concerning the Paper by Fung et al titled /’Differential Effects of Cyproterone Acetate vs Spironolactone on Serum High-Density Lipoprotein and Prolactin Concentrations in the Hormonal Treatment of Transgender Women/. Fung R, Lega I.J Sex Med. 2017 Jan;14(1):173-174. doi: 10.1016/j.jsxm.2016.11.306. No abstract available. PMID: 28065355 </br>7:Concerning the Article by Fung et al, Titled /Differential Effects of Cyproterone Acetate vs Spironolactone on Serum High-Density Lipoprotein and Prolactin Concentrations in the Hormonal Treatment of Transgender Women/. Defreyne J, T/’Sjoen G.J Sex Med. 2017 Jan;14(1):172-173. doi: 10.1016/j.jsxm.2016.10.014. No abstract available. PMID: 28065354 </br>8:Effects of antiandrogenic progestins, chlormadinone and cyproterone acetate, and the estrogen 17α-ethinylestradiol (EE2), and their mixtures: Transactivation with human and rainbowfish hormone receptors and transcriptional effects in zebrafish (Danio rerio) eleuthero-embryos. Siegenthaler PF, Bain P, Riva F, Fent K.Aquat Toxicol. 2017 Jan;182:142-162. doi: 10.1016/j.aquatox.2016.11.001. Epub 2016 Nov 9. PMID: 27907851 </br>9:Attenuation of the cyproterone acetate-induced testicular hypofunction by a novel nutraceutical lycopene: a genomic approach. Tripathy A, Ghosh A, Dey A, Pakhira BP, Ghosh D.Andrologia. 2016 Nov 24. doi: 10.1111/and.12709. [Epub ahead of print] PMID: 27882589 </br>10:Close follow-up after discontinuation of cyproterone acetate: a possible option to defer surgery in patients with voluminous intracranial meningioma. Zairi F, Aboukais R, LE Rhun E, Marinho P, Maurage CA, Lejeune JP.J Neurosurg Sci. 2017 Feb;61(1):98-101. No abstract available. PMID: 27857037 |
