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Mifepristone

Cat. No. M3510
Mifepristone Structure
Synonym:

RU486; C-1073; RU 38486

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
50mg USD 35  USD35 In stock
100mg USD 45  USD45 In stock
200mg USD 70  USD70 In stock
500mg USD 100  USD100 In stock
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Quality Control & Documentation
Biological Activity

Mifepristone (Mifeprex) is a competitive progesterone receptor antagonist with IC50 of 106 nM ,16 and 19 μg/ml for hog PR, HEC-1-A and Ishikawa, respectively. In the presence of progesterone, it acts as a competitive progesterone receptor antagonist (in the absence of progesterone, mifepristone acts as a partial agonist). It is a 19-nor steroid with a bulky p- (dimethylamino)phenyl substituent above the plane of the molecule at the 11β-position responsible for inducing or stabilizing an inactive receptor conformation and a hydrophobic 1-propynyl substituent below the plane of the molecule at the 17α-position that increases its progesterone receptor binding affinity.

Product Citations
Protocol (for reference only)
Cell Experiment
Cell lines OV2008 and SK-OV-3 cells
Preparation method Evaluating cell growth in various ovarian cancer cell lines that are subjected to dose-response or time course treatments.Replacing media containing each of the doses of fresh steroids every 24 hours. Treating control groups of cells with vehicle ethanol at a final concentration of less than 0.05%. Evluateing number of viable cells by trypsinization and counting in a hemocytometer chamber using trypan blue dye exclusion. Conducting experimentsin media without phenol red and supplemented with charcoal extracted fetal bovine serum, or media containing unextracted serum and having phenol red. Similar results are obtained with both media preparations; therefore, after performing the growth curves, using media with unextracted serum to conduct all subsequent experiments and in the presence of phenol red. When indicated, using software designed to study drug interaction to calculate the proliferation IC50s .
Concentrations 0-20 μM
Incubation time 24 hours
Animal Experiment
Animal models SK-OV-3 ovarian cancer cells are injected into immunosuppressed mice.
Formulation Constant release pellets (Innovative Research of America)
Dosages 0.5 or 1 mg/day
Administration Implanted s.c. with pellets
Chemical Information
Molecular Weight 429.59
Formula C29H35NO2
CAS Number 84371-65-3
Solubility (25°C) DMSO 76 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Eric A Schaff. Mifepristone: ten years later

[2] Courtney Schreiber, et al. Mifepristone in abortion care

[3] R M DeHart, et al. Mifepristone

[4] O Sartor, et al. Mifepristone: antineoplastic studies

[5] A Robbins, et al. Mifepristone: clinical pharmacology

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Keywords: Mifepristone, RU486; C-1073; RU 38486 supplier, Progesterone Receptor, inhibitors, activators


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