Ulipristal-acetate-CDB-2914-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEUlipristal acetateCat. No.: HY-16508CAS No.: 126784-99-4Synonyms: CDB-2914分式: CHNO分量: 475.62作靶点: Progesterone Receptor作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 33.33 mg/mL

2、(70.08 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.26 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.26 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Ulipristal acetate种选择性 体酮受体调节剂 (s

3、elective progesterone receptor modulator)，于治疗良性妇科疾病如宫肌瘤。体外研究 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 DNAfragmentation at the 100-ng/m

4、L dose and continuing up to the 10,000-ng/mL dose compared to thosespermatozoa in the control group 3.体内研究 Ulipristal and CDB-4124 have significant antiprogestational activity in vivo 1. Ulipristal acetate decreasesincidences of fibroadenomas and adenocarcinomas in the mammary gland in all treated g

5、roups. Ulipristalacetate exposure AUC(0-24h) at the highest dose in rats is 67 times human therapeutic exposure at 10mg/day. In mice, no tumor of any type increases at Ulipristal acetate exposures up to 313 times oftherapeutic exposure. Ulipristal acetate-related findings in mice are limited to orga

6、n weight changes in theliver, pituitary, thyroid/parathyroid glands, and epididymis as well as minimal panlobular hepatocellularhypertrophy 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 endometr

7、ium as being thickened compared tocontrols in a dose-dependent manner. There is a slight decrease in secretory differentiation with increasingdose of Ulipristal acetate, with small decreases in frequency of sub- and supra-nuclear vacuolation 5.PROTOCOLAnimal The study consisted of four groups, each

8、comprising four female cynomolgus monkeys. The groupsAdministration 5 eitherreceive ASV (control), or Ulipristal acetate at dose levels of 1, 5, or 25 mg/kg for 39 weeks. Twoadditional animals are allocated to the control and high dose groups for an 8-week post-dose recoveryperiod. At randomization,

9、 there is no statistically significant difference between treatment groups in meanbody weight. The vehicle or Ulipristal acetate is administered to all groups by oral gavage for 273consecutive days at a dose volume of 2 mL/kg. Following the dosing or recovery period, animals areeuthanized by intrave

10、nous administration of sodium pentobarbital followed by exsanguination of the femoralvessels.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Hum Reprod. 2015 Apr;30(4):800-11.See more customer validations on HYPERLINK / www.MedChemEREFERENCE

11、S1. Attardi BJ, et al. In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEmetabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone. J Steroid Biochem Mol Biol.

12、2004 Ma2. Ciarmela P, et al. Ulipristal acetate modulates the expression and functions of activin a in leiomyoma cells. Reprod Sci. 2014Sep;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 HealthCare. 2013

13、Oct;18(5):355-63.4. Pohl O, et al. Carcinogenicity and chronic rodent toxicity of the selective progesterone receptor modulator ulipristal acetate. Curr DrugSaf. 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.McePdf