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- Trilostane 13647-35-3

- Trilostane 13647-35-3
Trilostane 13647-35-3
产品描述 描述 Trilostane is an inhibitor of 3 beta-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome. It was withdrawn from the United States market in April 1994.
纯度 99%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 曲洛司坦;Win 24540外观 白色或类白色结晶性粉末可溶性/溶解性 DMSO : 60 mg/mL (182.1 mM)生物活性 靶点 3 β-hydroxysteroid dehydrogenaseIn vitro(体外研究) Both Trilostane and 4-Hydroxy tamoxifen (OHT) affects transcription of genes involved in cell cycle regulation, cell adhesion and matrix formation, however, only 12.5% of Trilostane down-regulated genes and 9.2% of up-regulated genes are similarly regulated by OHT in MCF-7 cells.?sup>In vivo(体内研究) Trilostane treatment results in a significant decline in basal plasma cortisol concentrations in dogs. Trilostane treatment results in an insignificant decrease in plasma aldosterone concentration (PAC), but the median plasma renin activity (PRA) at the time the trilostane dosage is considered optimal (265 fmol/L/s, range 70-3280 fmol/L/s; n=18) is significantly higher than prior to treatment (115 fmol/L/s, range 15-1330 fmol/L/s). Trilostane affects both the hypothalamic-pituitary-adrenocortical and the renin-aldosterone axes. Trilostane effectively blocks the increase in systolic blood pressure and reverses the hypertension produced by drinking 0.9% saline in the Dahlsalt-sensitive rat. Trilostane is equally effective in female and male rats. Trilostane reduces clinical signs and improves endocrine test results in all cats, but insulin requirements does not change and all continued to have some signs of hypercortisolemia. Trilostane results in a reduction in serum cortisol and aldosteroneconcentrations in dogs with PDH, although the decrease for serum aldosterone concentration is smaller than that for serum cortisol concentration.参考文献 参考文献 1. Puddefoot JR, et al. Expert Opin Pharmacother. 2006 Dec;7(17):2413-9.
2. Naville D, et al. Mol Endocrinol. 1991 Aug;5(8):1090-100.
3. Puddefoot JR, et al. Int J Cancer. 2002 Sep 1;101(1):17-22.
4. Barker S, et al. J Steroid Biochem Mol Biol. 2006 Aug;100(4-5):141-51.
4. Takahashi M, et al. J Steroid Biochem Mol Biol. 1990 Oct; 37(2):231-6.
研究领域 研究领域 Signal TransductionMetabolismDrug DiscoverySmall Molecule DrugLead Compound DiscoveryTrilostane 13647-35-3温馨提示:本产品仅作科研实验使用,不支持临床等研究
