Mifepristone
Modify Date: 2024-01-02 19:41:33
Mifepristone structure
|
Common Name | Mifepristone | ||
|---|---|---|---|---|
| CAS Number | 84371-65-3 | Molecular Weight | 429.594 | |
| Density | 1.2±0.1 g/cm3 | Boiling Point | 628.6±55.0 °C at 760 mmHg | |
| Molecular Formula | C29H35NO2 | Melting Point | 195-198°C | |
| MSDS | Chinese USA | Flash Point | 334.0±31.5 °C | |
| Symbol |
GHS08 |
Signal Word | Danger | |
Use of MifepristoneMifepristone is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay. |
| Name | mifepristone |
|---|---|
| Synonym | More Synonyms |
| Description | Mifepristone is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay. |
|---|---|
| Related Catalog | |
| Target |
IC50: 0.2 nM (progesterone receptor, in T47D cells), 2.6 nM (glucocorticoid receptor, in A549 cells)[1] |
| 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 Cisplatin is potentiated when administered in combination with Mifepristone in HeLa cells. The IC50 of Cisplatin in combination with Mifepristone is lower (14.2 μM) than that of Cisplatin alone (34.2 μM) in HeLa cells with an approximately 2.5-fold difference. After treatment with Mifepristone, the accumulation 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 μg/mg of protein[2]. |
| In Vivo | The cervix tumor xenograft models are treated with Cisplatin 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 Cisplatin 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 mg/dL). Subgroups of animals receive s.c. injection of Mifepristone (20 or 40 mg/kg in peanut oil). Although Mifepristone produces no significant changes in behavior of EtOH-naïve animals, pretreatment with Mifepristone (40 mg/kg) significantly reducesthe severity of EtOH withdrawal. Asignificant interaction between diet and drug, F(5,55)=3.92, p<0.05, such that EtOH-treated animals receiving vehicle or 20 mg/kg of Mifepristone displayssignificantly more signs of EtOH withdrawal than does EtOH-naïve animals receiving the same drug treatment. Importantly, treatment with 40 mg/kg of Mifepristone significantly reduces the severity of EtOH withdrawal, in a dose-dependent manner[3]. |
| Kinase Assay | T47D human breast cancer cells are plated in 96-well tissue culture plates at 10,000 cells per well in assay medium [RPMI medium without phenol red containing 5% (v/v) charcoal-treated FBS and 1% (v/v) penicillin-streptomycin]. Two days later, the medium is decanted and Mifepristone or control is added at a final concentration of 0.1% (v/v) dimethylsulfoxide in fresh assay medium. Twenty-four hours later, an alkaline phosphatase assay is performed using a SEAP kit. Briefly, the medium is decanted and the cells are fixed for 30 min at room temperature with 5% (v/v) formalin. The cells are washed once at room temperature with Hanks’ buffered saline solution. Equal volumes (0.05 mL) of 1× dilution buffer, assay buffer, and 1:20 substrate/enhancer mixture are then added. After a 1-h incubation at room temperature in the dark, the lysate is transferred to a white 96-well plate and luminescence is read using a LuminoSkan Ascent[1]. |
| Cell Assay | The HeLa and CaSki human cervical cancer cell lines are used. The effect of Mifepristone on proliferation of cells exposed to Cisplatin is evaluated using the XTT assay. The assay is based on the cleavage of the yellow tetrazolium salt XTT to form an orange formazan dye by metabolically active cells. The procedure is as follows. Cells are seeded into 96-well plates; Costar at a density of 6×103 viable cells per well in 100 μL culture medium. At the end of treatment with Cisplatin alone or the combination of Cisplatin plus Mifepristone, 50 μL XTT is added to each well (final concentration 0.3 mg/mL), follow by incubation for 4 h in a humidified atmosphere containing 5% CO2 at 37˚C. The absorbance of the samples is measured spectrophotometrically at 492 nm using a microtiter plate ELISA reader[2]. |
| Animal Admin | Mice[2] Female Nude mice between 6-8 weeks of age are implanted subcutaneously with 6×106 HeLa cells in a flank. Once tumors are ~5×5 mm, the animals are pair-matched into treatment and control groups. Each group consist of 8 tumor-bearing mice. The intraperitoneal administration of drugs or vehicle begin on day 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 combination study, the mice concurrently receive Cisplatin on the same schedule, and Mifepristone at the same dose 3 days previous to the administration of Cisplatin. The control animals receive only the vehicle. After administration of the drugs, mice are weighed and the tumors are measured with a caliper twice weekly. The tumor weight is calculated. Experiment is conducted for 74 days, after which time all animals are weighed and humanely euthanized. Rats[3] Adult male Sprague-Dawley rats, weighing between 224 and 245 g upon arrival, are used. Mifepristone (20 or 40 mg/kg) or vehicle (peanut oil) are administered subcutaneously (s.c.) once daily following the 0800 administration of EtOH or control diet. Mifepristone is suspended in peanut oil and sonicated for 30 minutes at least 24 hours prior to injection, it is then stored at 4°C until needed. Suspension is vortexed for 10 to 15 minutes prior to and as needed throughout dosing. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 628.6±55.0 °C at 760 mmHg |
| Melting Point | 195-198°C |
| Molecular Formula | C29H35NO2 |
| Molecular Weight | 429.594 |
| Flash Point | 334.0±31.5 °C |
| Exact Mass | 429.266785 |
| PSA | 40.54000 |
| LogP | 4.95 |
| Vapour Pressure | 0.0±1.9 mmHg at 25°C |
| Index of Refraction | 1.623 |
| Storage condition | 2-8°C |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
|
| Symbol |
GHS08 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H360 |
| Precautionary Statements | P201-P280-P308 + P313 |
| Personal Protective Equipment | Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges |
| Hazard Codes | T: Toxic; |
| Risk Phrases | R60 |
| Safety Phrases | S53-S22-S36/37/39-S45 |
| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |
| RTECS | KG2955000 |
| Precursor 0 | |
|---|---|
| DownStream 1 | |
CAS#:104004-96-8|
Potential role of hCG in apoptosis of human luteinized granulosa cells.
J. Reprod. Dev. 61(1) , 67-73, (2015) The corpus luteum (CL) forms after ovulation and acts as a temporary endocrine gland that produces progesterone (P4), a hormone that is essential for implantation and maintenance of pregnancy in mamma... |
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Disturbances in production of progesterone and their implications in plant studies.
Steroids 96 , 153-63, (2015) Progesterone is a mammalian hormone that has also been discovered in plants but its physiological function in plants is not explained. Experiments using inhibitors of progesterone synthesis and bindin... |
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Stress-Immune-Growth Interactions: Cortisol Modulates Suppressors of Cytokine Signaling and JAK/STAT Pathway in Rainbow Trout Liver.
PLoS ONE 10 , e0129299, (2015) Chronic stress is a major factor in the poor growth and immune performance of salmonids in aquaculture. However, the molecular mechanisms linking stress effects to growth and immune dysfunction is poo... |
| 11b-[4-(N,N-Dimethylamino)phenyl]-17a-(prop-1-ynyl)-D4,9-estradiene-17b-ol-3-one |
| (11β,17β)-11-[4-(Dimethylamino)phenyl]-17-hydroxy-17-(prop-1-yn-1-yl)estra-4,9-dien-3-one |
| (11β,17β)-11-[4-(dimethylamino)phenyl]-17-hydroxy-17-prop-1-yn-1-ylestra-4,9-dien-3-one |
| RU486 |
| (11b,17b)-11-[4-(Dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one |
| Estra-4,9-dien-3-one, 11-(4-(dimethylamino)phenyl)-17-hydroxy-17-(1-propynyl)-, (11β,17β)- |
| Estra-4,9-dien-3-one, 11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)-, (11b,17b)- |
| MFCD00867226 |
| Estra-4,9-dien-3-one, 11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(1-propyn-1-yl)-, (11β,17β)- |
| RU-486 |
| Mifepristone |
| (8S,11R,13S,14S,17S)-11-[4-(Dimethylamino)phenyl]-17-hydroxy-13-methyl-17-(1-propyn-1-yl)-1,2,6,7,8,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one |
| Mifestone |
| estra-4,9-dien-3-one, 11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)-, (11β,17β)- |
| 17-β-Hydroxy-11-β-(4-dimethylaminophenyl)-17-α-(1- propynyl)-estra-4,9-dien-3-one |
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