1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMifepristoneCat. No.: HY-13683CAS No.: 84371-65-3Synonyms: RU486; RU 38486分式: CHNO分量: 429.59作靶點(diǎn): Progesterone Receptor; Glucocorticoid Receptor; Autophagy作通路: Others; GPCR/G Protein; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn

2、 solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 59 mg/mL (137.34 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.3278 mL 11.6390 mL 23.2780 mL5 mM 0.4656 mL 2.3278 mL 4.6556 mL10 mM 0.2328 mL 1.1639 mL 2.3278 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請注意儲(chǔ)備液的保

3、存式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄的?chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.82 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 m

4、g/mL (5.82 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.82 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Mifepristone體酮受體 (PR) 和糖質(zhì)激素受體 (GR) 拮抗劑，體外實(shí)驗(yàn)中的 IC50 值分別為0.2 nM 和2.6nM。IC50 & Target IC50: 0.2 nM (progesterone recept

5、or, in T47D cells), 2.6 nM (glucocorticoid receptor, in A549 cells) 1體外研究 The discovery of the first competitive progesterone antagonist, Mifepristone, has stimulated an intensesearch for more potent and more selective antiprogestins 1. Cell growth is evaluated after 4 days ofexposure to Mifepriston

6、e at 10 M, a concentration close to the plasma concentration achievable in humans.The antiproliferative effect of Cisplatin is potentiated when administered in combination with Mifepristone inHeLa cells. The IC50 of Cisplatin in combination with Mifepristone is lower (14.2 M) than that of Cisplatina

7、lone (34.2 M) in HeLa cells with an approximately 2.5-fold difference. After treatment with Mifepristone, theaccumulation of intracellular Cisplatin in HeLa cells is 2-fold greater, representing a significant difference(p=0.009), compare with Cisplatin alone from 0.79 to 1.52 g/mg of protein 2.體內(nèi)研究

8、The cervix tumor xenograft models are treated with Cisplatin alone, there is a tumor growth inhibitioncompare with control group. However, the tumor weight loss is even more significant (p 2. Adult maleSprague-Dawley rats are subjected to a 4-day binge-like EtOH administration regimen (3 to 5 g/kg/i

9、.g. every8 hours designed to produce peak blood EtOH levels (BELs) of 3.PROTOCOLKinase Assay 1 T47D human breast cancer cells are plated in 96-well tissue culture plates at 10,000 cells per well in assaymedium RPMI medium without phenol red containing 5% (v/v) charcoal-treated FBS and 1% (v/v) penic

10、illin-streptomycin. Two days later, the medium is decanted and Mifepristone or control is added at a finalconcentration of 0.1% (v/v) dimethylsulfoxide in fresh assay medium. Twenty-four hours later, an alkalinephosphatase assay is performed using a SEAP kit. Briefly, the medium is decanted and the

11、cells are fixed for30 min at room temperature with 5% (v/v) formalin. The cells are washed once at room temperature withHanks buffered saline solution. Equal volumes (0.05 mL) of 1 dilution buffer, assay buffer, and 1:20substrate/enhancer mixture are then added. After a 1-h incubation at room temper

12、ature in the dark, the lysateis transferred to a white 96-well plate and luminescence is read using a LuminoSkan Ascent 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 2 The HeLa and CaSki human cervical cancer cell lines are used. The effe

13、ct of Mifepristone on proliferation ofcells exposed to Cisplatin is evaluated using the XTT assay. The assay is based on the cleavage of theyellow tetrazolium salt XTT to form an orange formazan dye by metabolically active cells. The procedure isas follows. Cells are seeded into 96-well plates; Cost

14、ar at a density of 6103 viable cells per well in 100 Lculture medium. At the end of treatment with Cisplatin alone or the combination of Cisplatin plus Mifepristone,2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE50 L XTT is added to each well (final concentration 0.3 mg/mL), follow by incubation f

15、or 4 h in a humidifiedatmosphere containing 5% CO2 at 37C. The absorbance of the samples is measured spectrophotometricallyat 492 nm using a microtiter plate ELISA reader 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 2Administration 23 F

16、emale Nude mice between 6-8 weeks of age are implanted subcutaneously with 6106 HeLa cells in aflank. Once tumors are 55 mm, the animals are pair-matched into treatment and control groups. Eachgroup consist of 8 tumor-bearing mice. The intraperitoneal administration of drugs or vehicle begin on day

17、0.Cisplatin, as a single agent, is administered intraperitoneally at a dose of 3 mg/kg daily on days 1 through 3;the dose of Mifepristone, as a single agent, is 2 mg/kg/day subcutaneously for 3 days; in the combinationstudy, the mice concurrently receive Cisplatin on the same schedule, and Mifeprist

18、one at the same dose 3days previous to the administration of Cisplatin. The control animals receive only the vehicle. Afteradministration of the drugs, mice are weighed and the tumors are measured with a caliper twice weekly. Thetumor weight is calculated. Experiment is conducted for 74 days, after

19、which time all animals are weighedand humanely euthanized.Rats 3Adult male Sprague-Dawley rats, weighing between 224 and 245 g upon arrival, are used. Mifepristone (20or 40 mg/kg) or vehicle (peanut oil) are administered subcutaneously (s.c.) once daily following the 0800administration of EtOH or co

20、ntrol diet. Mifepristone is suspended in peanut oil and sonicated for 30 minutesat least 24 hours prior to injection, it is then stored at 4C until needed. Suspension is vortexed for 10 to 15minutes prior to and as needed throughout dosing.MCE has not independently confirmed the accuracy of these me

21、thods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Sci Rep. 2017 Jul 26;7(1):6501. Biochem Biophys Res Commun. 2018 Jan 1;495(1):1108-1114. Gen Comp Endocrinol. 2018 Jul 1;263:51-61. Evid Based Complement Alternat Med. 2016;2016:5850739. Chinese Pharmacological Bulletin. 2017, 33(6): 878-882.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Jiang W,