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Ulipristal acetate

CAS No. : 126784-99-4

MCE 站：Ulipristal acetate

产品活性：Ulipristal acetate (CDB-2914) 是一种口服活性的选择性孕酮受体 (progesterone receptor) 调节剂 (SPRM)。Ulipristal acetate 选择性地刺激平滑肌瘤细胞的自噬反应。Ulipristal acetate 具有用于良性妇科疾病的潜力，如子宫肌瘤。

研究领域：Others  |  Autophagy

作用靶点：Progesterone Receptor  |  Autophagy

In Vitro: Ulipristal acetate (0.1-5 μM; 96 hours) stimulates autophagy in leiomyoma cells. Ulipristal-induced expression changes of the autophagic markers LC3 and p62/SQSTM1. Ulipristal up-regulates Atg7 protein in leiomyoma cells.
Ulipristal acetate blocks activin A modulation of fibronectin and vascular endothelial growth factor A (VEGF-A) mRNA expression in cultured myometrial and leiomyoma cells.

In Vivo: Ulipristal and CDB-4124 have significant antiprogestational activity in vivo.
Ulipristal acetate decreases incidences of fibroadenomas and adenocarcinomas in the mammary gland in all treated groups. Ulipristal acetate exposure [AUC(0-24h)] at the highest dose in rats is 67 times human therapeutic exposure at 10 mg/day. In mice, no tumor of any type increases at Ulipristal acetate exposures up to 313 times of therapeutic exposure. Ulipristal acetate-related findings in mice are limited to organ weight changes in the liver, pituitary, thyroid/parathyroid glands, and epididymis as well as minimal panlobular hepatocellular hypertrophy in male and female mice receiving 130 mg/kg/day.
Ulipristal acetate (1 mg/kg and 5 mg/kg) increases the frequency with which pathologists assessed the endometrium as being thickened compared to controls in a dose-dependent manner. There is a slight decrease in secretory differentiation with increasing dose of Ulipristal acetate, with small decreases in frequency of sub- and supra-nuclear vacuolation.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Endocrinology Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Breast Cancer Compound Library  |  Mifepristone  |  Progesterone  |  Medroxyprogesterone acetate  |  Cridanimod  |  Dydrogesterone  |  Dienogest  |  Tanaproget  |  Megestrol acetate  |  17α-Hydroxyprogesterone  |  Altrenogest  |  Nomegestrol acetate  |  Ulipristal  |  Drospire  |  Norethindrone  |  Desogestrel  |  Norethindrone acetate  |  Norethisterone enanthate  |  Chlormadi acetate  |  Ethynodiol diacetate  |  Medroxyprogesterone acetate D3  |  Nestoron  |  Asoprisnil  |  Estradiol dipropionate  |  Gestodene  |  Melengestrol acetate  |  Norgestimate  |  Tibolone  |  Gestonorone Capronate

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