Trimegestone  (Synonyms: RU 27987)

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^[1][2].

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.

342.47

C₂₂H₃₀O₃

74513-62-5

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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• [1]. Zhang Z, et al. In vitro characterization of trimegestone: a new potent and selective progestin. Steroids. 2000;65(10-11):637-643.  [Content Brief]

  [2]. Grubb G, et al. Clinical experience with trimegestone as a new progestin in HRT. Steroids. 2003;68(10-13):921-926.