中文名:曲洛司坦
CAS:13647-35-3
品牌:MedChemExpress (MCE)
存储条件:Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
生物活性:Trilostane(Win 24540; Modrastane) 是一种 3 β-羟基类固醇脱氢酶抑制剂,用于治疗库欣综合征。 IC50 值: 靶标:3 β-HSD Trilostane 是 3 β-羟基类固醇脱氢酶(3-β-HSD 或 delta 5-delta 4-异构酶)的抑制剂,是所有类激素类固醇生物合成的必需酶。它已被用于治疗库欣综合征以阻止皮质醇的产生,目前在美国被批准用于狗,但在英国和其他国家仍然是一种人类药物。正在研究将其作为乳腺癌和前列腺癌的可能治疗方法,以防止内源性前体合成雌激素和雄激素。它也被用于抑制研究中黄体酮的内源性产生。
体外:Trilostane 剂量和时间依赖性地影响肾上腺皮质孕烯醇酮代谢[2]。 Trilostane 选择性地抑制肾上腺中孕烯醇酮转化为孕酮[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内:Trilostane (5.3-50 mg/kg;口服,每天 1 次,持续 3 个月) 控制狗体内垂体依赖性的高肾上腺皮质激素含量[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Dogs with naturally-occurring pituitary-dependent hyperadrenocorticism (PDH)[1] Dosage: 5.3-50 mg/kg Administration: Oral administration; 5.3-50 mg/kg, once daily for 3 months Result: Effectively achieved endocrine control with safe effects and free of side-effects. Clinical Trial
参考详情:https://www.medchemexpress.com/Trilostane.html
参考文献:
[1]. JA Braddock, et al. Trilostane treatment in dogs with pituitary-dependent hyperadreno-corticism. Veterinary Journal. 10 March 2008.
[2]. Ouschan C, et al. The influence of trilostane on steroid hormone metabolism in canine adrenal glands and corpora lutea-an in vitro study. Vet Res Commun. 2012 Mar;36(1):35-40.