CAS NO: | 84371-65-3 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
100mg | 电议 |
500mg | 电议 |
1 g | 电议 |
5 g | 电议 |
生物活性 | Mifepristone (RU486) is aprogesterone receptor(PR) andglucocorticoid receptor(GR) antagonist withIC50s of 0.2 nM and 2.6 nM in in vitro assay[1]. | ||||||||||||||||
IC50& Target | IC50: 0.2 nM (progesterone receptor, in T47D cells), 2.6 nM (glucocorticoid receptor, in A549 cells)[1] | ||||||||||||||||
体外研究 (In Vitro) | The discovery of the first competitive progesterone antagonist, Mifepristone, has stimulated an intense search for more potent and more selective antiprogestins[1]. Cell growth is evaluated after 4 days of exposure to Mifepristone at 10 μM, a concentration close to the plasma concentration achievable in humans. The antiproliferative effect of NSC 119875 is potentiated when administered in combination with Mifepristone in HeLa cells. The IC50of NSC 119875 in combination with Mifepristone is lower (14.2 μM) than that of NSC 119875 alone (34.2 μM) in HeLa cells with an approximately 2.5-fold difference. After treatment with Mifepristone, the accumulation of intracellular NSC 119875 in HeLa cells is 2-fold greater, representing a significant difference (p=0.009), compare with NSC 119875 alone from 0.79 to 1.52 μg/mg of protein[2]. | ||||||||||||||||
体内研究 (In Vivo) | The cervix tumor xenograft models are treated with NSC 119875 alone, there is a tumor growth inhibition compare with control group. However, the tumor weight loss is even more significant (p<0.05) with the combination of NSC 119875 and Mifepristone at the doses used, showing a decrease of ~50% compared with the treatments alone by the end of the study[2]. Adult male Sprague-Dawley rats are subjected to a 4-day binge-like EtOH administration regimen (3 to 5 g/kg/i.g. every 8 hours designed to produce peak blood EtOH levels (BELs) of<300 mgdl). subgroups of animals receive s.c. injection mifepristone (20 or 40 kg inpeanut oil). although produces no significant changes behavior etoh-naive animals, pretreatment with (40 kg) significantly reducesthe severity etoh withdrawal. asignificantinteraction between diet and drug, f(5,55) =3.92, p<0.05, such that etoh-treated receiving vehicle 20 displayssignificantly more signs withdrawal than does the same drug treatment. importantly,treatment reduces withdrawal, a dose-dependent manner[3]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 429.59 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C29H35NO2 | ||||||||||||||||
CAS 号 | 84371-65-3 | ||||||||||||||||
中文名称 | 米非司酮;美服培酮 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(232.78 mM;ultrasonic and warming and heat to 60℃) 配制储备液
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以下溶剂前显示的百
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