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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.
Oncogenesis. 2024 Feb 29;13(1):10.
Progesterone receptor potentiates macropinocytosis through CDC42 in pancreatic ductal adenocarcinoma
Mifepristone purchased from AbMole
Oncogenesis. 2024 Feb 29;13(1).
Progesterone receptor potentiates macropinocytosis through CDC42 in pancreatic ductal adenocarcinoma
Mifepristone purchased from AbMole
bioRxiv. 2023 Jun.
Progesterone is an Inducement of Heritable Pulmonary Arterial Hypertension with BMPR2 Mutation
Mifepristone purchased from AbMole
BMC Med. 2021 Apr 7;19(1):87.
Dexamethasone induces an imbalanced fetal-placental-maternal bile acid circulation: involvement of placental transporters
Mifepristone purchased from AbMole
| 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 |
| 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 |
[1] Eric A Schaff. Mifepristone: ten years later
[2] Courtney Schreiber, et al. Mifepristone in abortion care
[3] R M DeHart, et al. Mifepristone
| Related Progesterone Receptor Products |
|---|
| PR antagonist 1
PR antagonist 1 is a selective progesterone receptor (PR) antagonist, and can be used for the research of a variety of progesterone-related diseases and disorders such as endometriosis and uterine fibroids. |
| Trimegestone
Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. |
| Nomegestrol
Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity. |
| Allylestrenol
Allylestrenol is an anabolic steroid with progesterone activity and potential physiologic function as a progesterone receptor agonist that can be used in studies related to preterm labor. |
| Cridanimod
Cridanimod is a potent progesterone receptor (PR) activator mediated through induction of IFNα and IFNβ expression. Cridanimod is a small-molecule immunomodulator and interferon inducer. |
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