Ulipristal Acetate

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Chemical Structure| 126784-99-4 同义名 : CDB-2914;HRP 2000;CDB-2914, CDB 2914, CDB2914, HRP-2000, HRP 2000, HRP2000, VA2914, VA-2914, VA 2914, RTI 3021-012, RU 44675, Ulipristal acetate, EllaOne, Ella, Esmya;RU 44675
CAS号 : 126784-99-4
货号 : A454107
分子式 : C30H37NO4
纯度 : 98%
分子量 : 475.619
MDL号 : MFCD00899035
存储条件：

Pure form Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(73.59 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Progesterone is a sex hormone that plays an important role in the pathogenesis of uterine leiomyomas. Ulipristal acetate is an orally active, selective progesterone receptor modulator that can stimulate autophagic response and upregulate Atg7 protein expression in leiomyoma cells at a concentration of 5µM (96 hours)[3]. The EC50 values of ulipristal acetate for recombinant human progesterone receptor-B, recombinant human progesterone receptor-A, rabbit uterine progesterone receptor, and rabbit thymic glucocorticoid receptor were 7.7±0.5, 8.5±0.6, 13.6±0.6, and 15.4±1.3nM, respectively[4]. In Sprague-Dawley rats, treatment with ulipristal acetate (1, 3, or 10mg/kg/day) decreased incidences of fibroadenomas and adenocarcinomas in the mammary gland[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.51mL

2.10mL

1.05mL

21.03mL

4.21mL

2.10mL
参考文献

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

[2]Attardi BJ, Burgenson J, 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 Mar;88(3):277-88.

[3]Del Bello B, Marcolongo P, Ciarmela P, et al. Autophagy up-regulation by ulipristal acetate as a novel target mechanism in the treatment of uterine leiomyoma: an in vitro study. Fertil Steril. 2019;112(6):1150-1159.

[4]Attardi BJ, Burgenson J, Hild SA, Reel JR. 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;88(3):277-288.

[5]Pohl O, Harvey PW, McKeag S, Boley SE, Gotteland JP. Carcinogenicity and chronic rodent toxicity of the selective progesterone receptor modulator ulipristal acetate. Curr Drug Saf. 2013;8(2):77-97.