Trimegestone
Trimegestone (RU 27987) is an orally active, selective progestogen and PR ligand, with an IC50 of 7.6 nM for hPR, 4.4 nM for rabbit PR, and 3.3 nM for rat PR. Trimegestone induces Alkaline phosphatase activity. Trimegestone exhibits antiandrogenic activity (IC50 = 303 nM). Trimegestone can be used in research related to menopausal symptoms and osteoporosis.
For research use only. We do not sell to patients.
- CAS No.: 74513-62-5
- Formula: C22H30O3
- Molecular Weight:342.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Trimegestone (variable dose; incubated overnight at 4°C) binds efficiently to hPR, rabbit and rat progesterone receptors, with the highest affinity for rat PR (IC50 = 3.3 nM)[1].
Trimegestone (24 h) dose-dependently increases alkaline phosphatase activity in T47D cells, with an EC50 of 0.09 nM, demonstrating potent progestogenic activity[1].
Trimegestone (0.001-0.1 nM; 24 h) stimulates the proliferation of T47D cells in a dose-dependent manner, with an EC50 of 0.02 nM, exhibiting potent progestogenic activity[1].
Trimegestone (0.001-10 nM) induces HRE-tk-luciferase activity in a dose-dependent manner in HESC-T cells that transiently express ER (and induce PR expression), with an EC50 of 0.2 nM, but shows no activity in PR-negative HESC-T cells[1].
Trimegestone (0-10000 nM; 24 h) exhibits negligible androgenic activity but shows antiandrogenic activity (IC50 = 303 nM) in AR-positive, PR-negative L929 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human T47D breast carcinoma cells
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Concentration:0.001-0.1 nM
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Incubation Time:24 h
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Result:Increased T47D cell proliferation in a dose-dependent manner, with a mean EC50 of 0.02 nM, matching the potency of medroxyprogesterone acetate.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 74513-62-5
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Molecular Weight 342.47
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Formula C22H30O3
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SMILES
C[C@@]12[C@](CC[C@]2(C)C([C@@H](O)C)=O)([H])[C@@]3([H])C(CC1)=C4C(CC3)=CC(CC4)=O
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Synonyms
RU 27987
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)