| Size | Price | |
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| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| Targets |
Trimegestone targets the progesterone receptor (PR). It acts as a highly potent agonist, binding to the PR and activating its transcriptional activity. This leads to the regulation of gene expression, resulting in the secretory transformation of the endometrium, which is essential for endometrial protection during estrogen therapy. The compound has an IC50 of 3.3 nM for the rat PR, indicating its high affinity. It also increases alkaline phosphatase activity, with an EC50 of 0.1 nM, but does not increase luciferase activity, suggesting a complex mechanism of action that may involve selective activation of specific PR-mediated pathways.
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| ln Vitro |
In vitro, trimegestone has been shown to be a potent agonist of the progesterone receptor. It binds to the PR with high affinity and induces the expression of progesterone-responsive genes. In cell-based assays using cells expressing the PR, the compound stimulates alkaline phosphatase activity. This activity is a marker of progestogenic activity. The compound's ability to induce secretory transformation of the endometrium has been confirmed in vitro using endometrial cell lines or primary cultures.
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| ln Vivo |
In vivo, trimegestone is effective in providing endometrial protection in postmenopausal women receiving estrogen therapy. It induces secretory transformation of the endometrium, preventing the endometrial hyperplasia that can occur with unopposed estrogen use. The compound is used in menopausal hormone therapy for this purpose. It is also used in the prevention of postmenopausal osteoporosis. The compound's high potency and oral activity make it a convenient and effective option for hormone replacement therapy.
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| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for trimegestone involve studying its binding affinity for the progesterone receptor. These assays use a radioligand binding method with membrane preparations from cells expressing the PR (e.g., rat PR). The compound is incubated with a radiolabeled ligand, such as [3H]progesterone or [3H]ORG 2058, and the displacement of the ligand is measured to determine the IC50 or Ki. For trimegestone, an IC50 of 3.3 nM for the rat PR has been reported. Selectivity is assessed by testing the compound against other steroid receptors, such as estrogen, androgen, and glucocorticoid receptors.
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| Cell Assay |
In vitro cell-based assays for trimegestone are performed using cells that express the progesterone receptor, such as T47D breast cancer cells or endometrial cell lines. Cells are treated with the compound, and the expression of progesterone-responsive genes is measured by qPCR or reporter gene assays. Alkaline phosphatase activity is measured as a marker of progestogenic activity. Cell proliferation assays can also be used to assess the compound's effects on cell growth. These assays confirm the compound's agonist activity at the PR.
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| Animal Protocol |
In vivo animal experiments for trimegestone are conducted using rodent models of endometrial hyperplasia and osteoporosis. Ovariectomized rats are used to model postmenopausal conditions. The compound is administered orally, and its effects on the endometrium and bone are assessed. Endometrial thickness, histology, and the expression of progesterone-responsive genes are evaluated. Bone mineral density and bone turnover markers are measured to assess the compound's efficacy in preventing osteoporosis.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of trimegestone indicate that it is orally active and has good bioavailability. The compound has a molecular weight of 342.47 and a molecular formula of C22H30O3. It is a solid at room temperature. The powder is stable when stored at -20°C for up to 3 years. The compound is metabolized in the liver, and its half-life is suitable for once-daily dosing. Its pharmacokinetic profile is characterized by good absorption and a predictable elimination pattern.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for trimegestone indicate that it is generally well-tolerated. As a progestogen, its side effects are similar to those of other progestins and may include breast tenderness, mood changes, and breakthrough bleeding. It has a favorable metabolic profile compared to some other progestins, with minimal effects on lipid and glucose metabolism. The compound is not associated with significant hepatotoxicity or other serious adverse effects at therapeutic doses.
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| References | |
| Additional Infomation |
Trimegristone is a 20-oxosteroid. Trimegristone has been used in clinical trials to investigate the treatment of diseases in postmenopausal women.
Other information: Trimegestone is a highly effective oral progestogen used in menopausal hormone therapy and for endometrial protection. It is also known as RU 27987. The compound is being studied for its potential in contraception and other applications. Its CAS number is 74513-62-5. |
| Molecular Formula |
C22H30O3
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|---|---|
| Molecular Weight |
342.47
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| Exact Mass |
342.219
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| CAS # |
74513-62-5
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| PubChem CID |
68926
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
522.6±50.0 °C at 760 mmHg
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| Flash Point |
284.0±26.6 °C
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| Vapour Pressure |
0.0±3.1 mmHg at 25°C
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| Index of Refraction |
1.569
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| LogP |
3.58
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
700
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O=C1CCC2=C3CC[C@@]4([C@@](CC[C@H]4[C@@H]3CCC2=C1)(C)C([C@@H](O)C)=O)C
|
| InChi Key |
JUNDJWOLDSCTFK-MTZCLOFQSA-N
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| InChi Code |
InChI=1S/C22H30O3/c1-13(23)20(25)22(3)11-9-19-18-6-4-14-12-15(24)5-7-16(14)17(18)8-10-21(19,22)2/h12-13,18-19,23H,4-11H2,1-3H3/t13-,18+,19-,21-,22+/m0/s1
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| Chemical Name |
(8S,13S,14S,17S)-17-[(2S)-2-hydroxypropanoyl]-13,17-dimethyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one
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| Synonyms |
RU-27987 RU 27987 Trimegestone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9200 mL | 14.5998 mL | 29.1996 mL | |
| 5 mM | 0.5840 mL | 2.9200 mL | 5.8399 mL | |
| 10 mM | 0.2920 mL | 1.4600 mL | 2.9200 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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