126784-99-4

• 常用中文名：醋酸乌利司他
• 常用英文名：Ulipristal acetate
• CAS号：126784-99-4
• 分子式：C₃₀H₃₇NO₄
• 分子量：475.619
• 相关类别： 原料药 激素及调节内分泌功能类药 避孕药
• 发布时间：2018-07-26 22:47:34
• 更新时间：2026-07-01 18:14:10
• Ulipristal acetate 是一种选择性黄体酮受体调节剂 (selective progesterone receptor modulator)，用于治疗良性妇科疾病如子宫肌瘤。

名称

• 中文名: (11b)-17-(乙酰氧基)-11-[4-(二甲基氨基)苯基]-19-去甲孕甾-4,9-二烯-3,20-二酮
• 英文名: ulipristal acetate
• 中文别名: 醋酸乌利司他,10 MM DMSO 溶液; 醋酸乌利司酮; 醋酸优力思特; 醋酸优力司特; 醋酸乌利司他/醋酸优力司特/CDB2914; 醋酸乌利斯他; 醋酸乌立司他; 优力斯特; 醋酸乌利司他杂质C1; 醋酸乌利司他(微粉级); ULIPRISTAL|||醋酸乌利司他|||CDB-2914; 醋酸乌利司他|原料药126-4; 17Α-乙酰氧基-11Β-(4-N,N-二甲氨基苯基)19-去甲孕甾-4,9-二烯-3,20-二酮; 醋酸优力斯特(乌利司他; 醋酸尤利司特; 醋酸乌利司他标准品004; (11B)-17-(乙酰氧基)-11-[4-(二甲基氨基)苯基]-19-去甲孕甾-4,9-二烯-3,20-二酮; 醋酸乌利司他/醋酸优力司特; 优力司特; (8S,11R,13S,14S,17R)-3-氧代-11-[4-(二甲氨基)苯基]-13-甲基-17-乙酰基-2,3,6,7,8,11,12,13,14,15,16,17-十二氢-1H-环戊并[A]菲-17-基乙酸酯; (11Β)-17Α-(乙酰氧基)-11-[4-(二甲基氨基)苯基]-19-去甲孕甾-4,9-二烯-3,20-二酮; (8S,11R,13S,14S,17R)-17-乙酰基-11-(4-(二甲基氨基)苯基)-13-甲基-3-氧代-2,3,6,7,8,11,12,13 ,14,15,16,17-十二氢-1H-环戊二烯并[A]菲-17-基乙酸酯; 醋酸乌利司他杂质4; 醋酸乌利妥; (11Β)-17-(乙酰氧基)-11-[4-(二甲基氨基)苯基]-19-去甲孕甾-4,9-二烯-3,20-二酮; 醋酸优力斯特; 醋酸乌里司他; (11B)-17-(乙酰氧基)-CHEMICALBOOK11-[4-(二甲基氨基)苯基]-19-去甲孕甾-4,9-二烯-3,20-二酮
• 英文别名: Ulipristal Actate; Ulipristal acetate, >=; Ulipristal acetateQ: What is Ulipristal acetate Q: What is the CAS Number of Ulipristal acetate Q: What is the storage condition of Ulipristal acetate Q: What e the applications of Ulipristal acetate; (11β)-17-(Acetyloxy)-11-[4-(dimethylamino)phenyl]-19-norpregna-4,9-diene-3,20-dione; Ulipristal acetate, 10 mM in DMSO; (11b)-17-(Acetyloxy)-11-[4-(dimethylamino)phenyl]-19-norpregna-4,9-diene-3,20-dione; Ulipristal,Ella; (11β)-17-(Acetyloxy)-11-(4-(dimethylamino)phenyl)-19-norpregna-4,9-diene-3,20-dione; (8S,11R,13S,14S,17R)-17-Acetyl-11-(4-(dimethylamino)phenyl)-13-methyl-3-oxo-2,3,6,7,8,11,12,13; (11β)-11-[4-(Dimethylamino)phenyl]-3,20-dioxo-19-norpregna-4,9-dien-17-yl acetate; Ulipristal Acetate 126-4; 19-Norpregna-4,9-diene-3,20-dione, 17-(acetyloxy)-11-[4-(dimethylamino)phenyl]-, (11β); Ella; Ulipristal acetate/CDB2914; 17α-Acetoxy-11β-(4-dimethylaminophenyl)-19-norpregna-4,9-dien-3,20-dione; 17a-Acetoxy-11b-[4-N,N-diMethylaMinophenyl]-19-norpregna-4,9-diene-3,20-dione; CDB2914(Uliprisnil acetate); Ulipristal acetate,Ella; Ullistat acetate; top quality Ulipristal Acetate; Esmya; 17alpha-Acetoxy-11beta-[4-(diMethylaMino)phenyl]-19-norpregna-4,9-diene-3,20-dione; Ulipristal-004; 19-Norpregna-4,9-diene-3,20-dione,17-(acetyloxy)-11-[4-(diMethylaMino)phenyl]-, (11b); 17alpha-Acetoxy-11beta-[4-(dimethylamino)phenyl]-19-norpregn; CDB2914; Uliprisnil acetate(CDB2914); Ulipristal Acetate Impurity4; Uliste acetate; Ulipristal Acetate //BP; EllaOne; (8S,11R,13S,14S,17R)-17-Acetyl-11-(4-(dimethylamino)phenyl)-13-methyl-3-oxo-2,3,6,7,8,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl acetate; [(8S,11R,13S,14S,17R)-17-acetyl-11-[4-(dimethylamino)phenyl]-13-methyl-3-oxo-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-17-yl] acetate; (11beta)-17-(Acetyloxy)-11-[4-(dimethylamino)phenyl]-19-norpregna-4,9-diene-3,20-dione; (11β)-(17-Acetyloxy)-11-[4-(dimethylamino)-phenyl]-19-norpregna-4,9-diene-3,20-dione; Ulipristal (acetate); (8S,11R,13S,14S,17R)-17-acetyl; Uliprisnil Acetate; VA2914; Ulipristal; Acetaldehyde ester; CDB-2914; 17α-Acetoxy-11β-[4-N,N-dimethylaminophenyl]-19-norpregna-4,9-diene-3,20-dione

物化性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 640.1±55.0 °C at 760 mmHg
• 熔点: 183-185ºC
• 分子式: C₃₀H₃₇NO₄
• 分子量: 475.619
• 闪点: 340.9±31.5 °C
• 精确质量: 475.272247
• PSA: 63.68000
• LogP: 4.48
• 外观性状: 固体;White to Yellow to Green powder to crystal
• 蒸汽压: 0.0±1.9 mmHg at 25°C
• 折射率: 1.594
• 储存条件: -20°C

生物活性

• 描述: Ulipristal acetate 是一种选择性黄体酮受体调节剂 (selective progesterone receptor modulator),用于治疗良性妇科疾病如子宫肌瘤。
• 相关类别:
  信号通路 >> 其他 >> 孕激素受体
  研究领域 >> 内分泌
• 体外研究: Ulipristal acetate阻断激活素A对培养的子宫肌层和平滑肌瘤细胞中纤维连接蛋白和血管内皮生长因子A(VEGF-A)mRNA表达的调节[2]。与对照组中的那些精子相比,醋酸乌利司他降低了100-ng/mL剂量的DNA片段化并持续至10,000-ng/mL剂量[3]。
• 体内研究: Ulipristal和CDB-4124在体内具有显着的抗孕活性[1]。醋酸乌利司他降低了所有治疗组乳腺中纤维腺瘤和腺癌的发生率。在大鼠中最高剂量的醋酸乌利司他暴露[AUC(0-24h)]是10mg /天的人治疗暴露的67倍。在小鼠中,在Ulipristal醋酸盐暴露下,任何类型的肿瘤都没有增加,达到治疗暴露的313倍。小鼠醋酸乌利司他相关的发现仅限于肝脏,垂体,甲状腺/甲状旁腺和附睾的器官重量变化以及接受130 mg/kg /天的雄性和雌性小鼠的最小小叶肝细胞肥大[4]。醋酸乌利司他(1 mg/kg和5 mg/kg)增加了病理学家评估子宫内膜增厚的频率,与对照组相比,呈剂量依赖性。随着醋酸Ulipristal剂量的增加,分泌分化略有下降,亚核和超核空泡化频率略有下降[5]。
• 动物实验: 该研究由四组组成，每组包括四只雌性食蟹猴。这些组以1,5或25mg / kg的剂量水平接受ASV（对照）或醋酸乌利司他，持续39周。另外两只动物分配给对照和高剂量组，用于给药后8周的恢复期。在随机化中，治疗组之间在平均体重方面没有统计学上的显着差异。通过口服管饲法以2mL / kg的剂量体积将载体或醋酸乌利司他施用于所有组连续273天。在给药或恢复期后，通过静脉内给予戊巴比妥钠然后放血股动脉使动物安乐死。
• 参考文献:

  [1]. Attardi BJ, et al. In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone. J Steroid Biochem Mol Biol. 2004 Ma

  [2]. Ciarmela P, et al. Ulipristal acetate modulates the expression and functions of activin a in leiomyoma cells. Reprod Sci. 2014 Sep;21(9):1120-5.

  [3]. Munuce MJ, et al. Effects of ulipristal acetate on sperm DNA fragmentation during in vitro incubation. Eur J Contracept Reprod Health Care. 2013 Oct;18(5):355-63.

  [4]. Pohl O, et al. Carcinogenicity and chronic rodent toxicity of the selective progesterone receptor modulator ulipristal acetate. Curr Drug Saf. 2013 Apr;8(2):77-97.

  [5]. Pohl O, et al. A 39-week oral toxicity study of ulipristal acetate in cynomolgus monkeys. Regul Toxicol Pharmacol. 2013 Jun;66(1):6-12.

安全

• 符号: GHS08
• 信号词: Warning
• 危害声明: H361fd
• 警示性声明: P280
• 危害码 (欧洲): Xi
• 危险品运输编码: NONH for all modes of transport

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