醋酸乌利司他 T2527

Product Introduction
Bioactivity


英文名: Ulipristal acetate

描述: Ulipristal acetate (CDB-2914) 是一种具有抗孕酮活性的选择性孕酮受体调节剂。它可抑制子宫平滑肌瘤病的生长。它通过抑制或延迟排卵和影响子宫内膜组织，可用作紧急避孕药。

体外活性: Ulipristal acetate blocks activin A modulation of fibronectin and vascular endothelial growth factor A (VEGF-A) mRNA expression in cultured myometrial and leiomyoma cells[2]. Ulipristal acetate decreases the DNA fragmentation at the 100-ng/mL dose and continuing up to the 10,000-ng/mL dose compared to those spermatozoa in the control group[3].

体内活性: Ulipristal and CDB-4124 have significant antiprogestational activity in vivo[1]. 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, there is no increase in tumors of any type at Ulipristal acetate exposures up to 313 times 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[4]. 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[5].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (105.12 mM)


关键字: NR3C3 | inhibit | CDB2914 | Ulipristal Acetate | Ulipristal acetate | anti-fertility | anti-glucocorticoid | CDB 2914 | Autophagy | Inhibitor | anti-progestational | contraception | leiomyoma | uterine | emergency | Progesterone Receptor

相关产品: (R)-Equol | Ethynodiol diacetate | Pregnanediol | Psoralidin | SR 19881 | Iriflophenone | (±)-Equol | 27-Hydroxycholesterol | OBHSA | SIM-688

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | EMA Approved Drug Library | Target-Focused Phenotypic Screening Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途