Cyproterone acetate-d3 is deuterium labeled Cyproterone acetate. Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors[1][2].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
419.96
Formula
C24H26D3ClO4
CAS 号
2376035-90-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. 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.
[3]. Torri V,. Cyproterone acetate in the therapy of prostate carcinoma. Arch Ital Urol Androl. 2005;77(3):157-163.
[4]. Chen L, et al. Cyproterone acetate enhances TRAIL-induced androgen-independent prostate cancer cell apoptosis via up-regulation of death receptor 5. BMC Cancer. 2017;17(1):179. Published 2017 Mar 7.
[5]. Takiguchi M, et al. Cyproterone acetate induces a cellular tolerance to cadmium in rat liver epithelial cells involving reduced cadmium accumulation. Toxicology. 2001;165(1):13-25.
[6]. Migally N. Effect of cyproterone acetate on the structure of the adrenal cortex. Arch Androl. 1979;2(2):109-115.
Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors[1][2].
体外研究 (In Vitro)
Cyproterone acetate is a partial agonist, showing agonism for the AR, with EC50 of 4.0 μM, at relatively high concentrations[1]. Cyproterone acetate enhances TRAIL-induced androgen-independent prostate cancer cell apoptosis via up-regulation of death receptor 5[3]. Cyproterone acetate pretreatment (0,1,10, or 50 μM; 24 hours; subsequently exposed to cadmium for an additional 24 hours) resulted in a clear decrease in the sensitivity to cadmium in rat liver epithelial cell line[4].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Adult male C57 BL/6J mice injected with 0.08 mg/g of cyproterone acetate showed an increase in cellular lipid content in the zona fasciculata and zona retjculans of the adrenal cortex[5].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
402.91
Formula
C23H27ClO4
CAS 号
427-51-0
中文名称
醋酸环丙孕酮;色普龙
运输条件
Room temperature in continental US; may vary elsewhere.
[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]. Torri V,. Cyproterone acetate in the therapy of prostate carcinoma. Arch Ital Urol Androl. 2005;77(3):157-163.
[3]. Chen L, et al. Cyproterone acetate enhances TRAIL-induced androgen-independent prostate cancer cell apoptosis via up-regulation of death receptor 5. BMC Cancer. 2017;17(1):179. Published 2017 Mar 7.
[4]. Takiguchi M, et al. Cyproterone acetate induces a cellular tolerance to cadmium in rat liver epithelial cells involving reduced cadmium accumulation. Toxicology. 2001;165(1):13-25.
[5]. Migally N. Effect of cyproterone acetate on the structure of the adrenal cortex. Arch Androl. 1979;2(2):109-115.