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Mifepristone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Mifepristone图片
CAS NO:84371-65-3
包装与价格:
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

产品名称
米非司酮
RU486
RU 38486
产品介绍
Mifepristone (RU486) 是黄体酮受体 (PR) 和糖皮质激素受体 (GR) 拮抗剂,体外实验中的IC50值分别为 0.2 nM 和 2.6 nM。
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
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3278 mL11.6390 mL23.2780 mL
5 mM0.4656 mL2.3278 mL4.6556 mL
10 mM0.2328 mL1.1639 mL2.3278 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂: 0.5%CMC-Na/saline water

    Solubility: 10 mg/mL (23.28 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.82 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.82 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.82 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。