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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 74513-62-5
- 分子式: C22H30O3
- 分子量:342.47
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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 |
化学情報
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CAS 番号 74513-62-5
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分子量 342.47
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分子式 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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別名
RU 27987
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)