Mifepristone

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Chemical Structure| 84371-65-3 同义名 : RU 38486;RU486;Corlux.;Mifepristona;Mifepristonum;Brand name: Mifegyne；Mifepriston；Pictovir;C-1073
CAS号 : 84371-65-3
货号 : A423786
分子式 : C29H35NO2
纯度 : 99+%
分子量 : 429.59
MDL号 : MFCD00867226
存储条件：

Pure form Inert atmosphere,2-8°C

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

DMSO: 105 mg/mL(244.42 mM)，配合低频超声，并水浴加热至45℃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
靶点

  • Progesterone receptor

    Progesterone receptor, IC50:0.2 nM
描述 Mifepristone (RU486) acts as an antagonist for both progesterone receptor (PR) and glucocorticoid receptor (GR), displaying IC50 values of 0.2 nM and 2.6 nM, respectively, in in vitro assays[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A549 cells Function assay Antagonist activity at human glucocorticoid receptor assessed as inhibition of corticoid-induced transcription in human A549 cells by GRE-linked luciferase reporter gene assay, IC50=0.0016 μM 17317167
A549 cells Function assay 16 h Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced transcription after 16 hrs by glucocorticoid response element-driven luciferase reporter gene assay, IC50=0.0016 μM 19217285
CHO cells Function assay Inhibition of Dexamethasone stimulated transcriptional activity in CHO cells expressing glucocorticoid receptor, IC50=0.005 μM 12824023
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01419535 Endocrine Disease ... 展开 >> Diabetes 收起 << Phase 1 Phase 2 Completed - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<
NCT01898312 Women With Mutations in the Br... 展开 >>east Cancer Susceptibility Genes BRCA1,2 收起 << Phase 2 Recruiting December 2018 Sweden ... 展开 >> Department of Woman and Child Health Karolinska University Hospital Recruiting Stockholm, Sweden, 17176 Sub-Investigator: Angelique Flöter Rådestad, MD PhD 收起 <<
NCT00382538 Abortion, Induced ... 展开 >> Abortion, Second Trimester 收起 << Not Applicable Completed - United States, Massachusetts ... 展开 >> Boston Medical Center Boston, Massachusetts, United States, 02118 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.64mL

2.33mL

1.16mL

23.28mL

4.66mL

2.33mL
参考文献

[1]Jiang W, et al. New progesterone receptor antagonists: phosphorus-containing 11beta-aryl-substituted steroids. Bioorg Med Chem. 2006 Oct 1;14(19):6726-32.

[2]Jurado R, et al. NSC 119875 cytotoxicity is increased by mifepristone in cervical carcinoma: an in vitro and in vivo study. Oncol Rep. 2009 Nov;22(5):1237-45.

[3]Sharrett-Field L, et al. Mifepristone Pretreatment Reduces Ethanol Withdrawal Severity In Vivo. Alcohol Clin Exp Res. 2013 Aug;37(8):1417-23.