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/ Mifepristone/米非司酮

Mifepristone/米非司酮 {[allProObj[0].p_purity_real_show]}

货号：A423786 同义名： RU 38486; RU486

Mifepristone is an antagonist of progesterone receptor (IC50 = 0.2 nM) and glucocorticoid receptor (IC50 = 2.6 nM).

Mifepristone/米非司酮 化学结构 CAS号：84371-65-3
Mifepristone/米非司酮 化学结构
CAS号：84371-65-3
Mifepristone/米非司酮 3D分子结构
CAS号：84371-65-3
Mifepristone/米非司酮 化学结构 CAS号：84371-65-3
Mifepristone/米非司酮 3D分子结构 CAS号：84371-65-3
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Mifepristone/米非司酮 纯度/质量文件 产品仅供科研

货号：A423786 标准纯度： {[allProObj[0].p_purity_real_show]}
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Mifepristone/米非司酮 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].

Mifepristone/米非司酮 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 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
CHO-K1 cells Function assay Inhibition of CHO-K1 cells expressing glucocorticoid receptor, IC50=8e-06 μM 15456242

Mifepristone/米非司酮 动物研究

Animal study In cervix tumor xenograft models treated with NSC 119875 alone, there is notable tumor growth inhibition compared to the control group. However, combining NSC 119875 with Mifepristone results in even more significant tumor weight reduction (p<0.05), achieving approximately a 50% decrease compared to individual treatments by the study's end[2].Adult male Sprague-Dawley rats undergo a 4-day binge-like ethanol (EtOH) administration regimen (3 to 5 g/kg, orally, every 8 hours), aimed at achieving peak blood EtOH levels (BELs) under 300 mg/dL. Subgroups of these animals receive subcutaneous injections of Mifepristone (20 or 40 mg/kg in peanut oil). While Mifepristone does not significantly alter the behavior of EtOH-naïve animals, pretreatment with Mifepristone (40 mg/kg) significantly reduces the severity of EtOH withdrawal. There is a notable interaction between diet and drug, F(5,55)=3.92, p<0.05, showing that EtOH-treated animals receiving either the vehicle or 20 mg/kg of Mifepristone exhibit significantly more signs of EtOH withdrawal compared to EtOH-naïve animals undergoing the same treatment. Crucially, 40 mg/kg of Mife

Mifepristone/米非司酮 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 <<

Mifepristone/米非司酮 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.

Mifepristone/米非司酮 实验方案

计算器
存储液制备 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

Mifepristone/米非司酮 技术信息

CAS号84371-65-3
分子式C29H35NO2
分子量 429.59
SMILES Code C[C@@]12[C@@](C#CC)(O)CC[C@@]1([H])[C@]3([H])CCC4=CC(CCC4=C3[C@@H](C5=CC=C(N(C)C)C=C5)C2)=O
MDL No. MFCD00867226
别名 RU 38486; RU486; Mifepristona; Mifepristonum; C-1073
运输蓝冰
InChI Key VKHAHZOOUSRJNA-GCNJZUOMSA-N
Pubchem ID 55245
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二

Tags: Mifepristone | 84371-65-3 | RU486 | RU 38486 | RU 486 | RU-486 | RU38486 | RU 38486 | RU-38486 | Progesterone Receptor Antagonist | Vitamin D Related/Nuclear Receptor | Immunology/Inflammation | Autophagy | Progesterone Receptor | Glucocorticoid Receptor | NO Synthase | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Mifepristone/米非司酮 纯度/质量文件 | Mifepristone/米非司酮 生物活性 | Mifepristone/米非司酮 细胞研究 | Mifepristone/米非司酮 临床数据 | Mifepristone/米非司酮 参考文献 | Mifepristone/米非司酮 实验方案 | Mifepristone/米非司酮 技术信息

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