Nomegestrol acetate
Based on 1 Customer Validation
Nomegestrol acetate is an orally active, highly selective progestogen and a progesterone receptor complete agonist. Nomegestrol acetate inhibits ovulation. Nomegestrol acetate is also effective in inhibiting the proliferation of human endometrial cancer RL95-2 cells in vitro and in vivo. Nomegestrol acetate can be used in cancer (especially endometrial cancer) and contraceptive studies.
For research use only. We do not sell to patients.
- Purity: 99.73%
- CAS No.: 58652-20-3
- Formula: C23H30O4
- Molecular Weight:370.48
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Progesterone receptor[3].
Nomegestrol acetate (0.3, 1, 3, 10, 30, 100 µM; 24, 48, 72 h) shows anti-proliferative activity against RL95-2 cells in a dose-dependent manner[1].
Nomegestrol acetate (4, 20, 100 µM; 6, 24, 48 h) upregulates protein levels of SUFU and Wnt7a in RL95-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RL95-2 cells
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Concentration:0.3, 1, 3, 10, 30, and 100 µM
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Incubation Time:24, 48, 72 h
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Result:Inhibited the growth of RL95-2 cells in a concentration-dependent manner, with IC50 values of 19.88, 21.62 and 52.80 µM for 48, 72 and 24 h.
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Cell Line:RL95-2 cells
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Concentration:4, 20, 100 µM
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Incubation Time:6, 24, 48 h
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Result:Increased the protein levels of SUFU and Wnt7a (relative to GAPDH expression) in a concentration-dependent manner.
Nomegestrol acetate (100, 200 mg/kg; p.o.; single daily for 28 days) surpresses the expression of SUFU and Wnt7a in tumor tissues[1].
Nomegestrol acetate (1, 2.5 mg/rat; p.o.; single daily for 4 days) inhibits ovulation in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic nude mice (BALB/c; 18-20 g; 6 to 7-week-old; xenograft nude mouse model)[1].
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Dosage:50, 100, 200 mg/kg
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Administration:Oral gavage; single daily for 28 days
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Result:Reduced the growth of RL95-2 xenograft tumors in vivo.
Upregulated the expression of SUFU and Wnt7a in a dose-dependent manner when at 100 and 200 mg/kg.
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Animal Model:Mature female Wistar rats (~200 g)[2].
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Dosage:1, 2.5 mg/rat
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Administration:Oral administration; single daily for 4 days
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Result:Showed only one animal ovulated after receiving 1 mg/kg per day, and no animals ovulated after receiving 2.5 mg/rat per day.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 58652-20-3
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Appearance Solid
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Molecular Weight 370.48
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Formula C23H30O4
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Color White to off-white
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SMILES
CC([C@@]1(OC(C)=O)CC[C@@]2([H])[C@]3([H])C=C(C)C4=CC(CC[C@]4([H])[C@@]3([H])CC[C@]12C)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 62.5 mg/mL (168.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (622 KB)
- English - EN (622 KB)
- Français - FR (622 KB)
- Deutsch - DE (622 KB)
- Norwegian - NO (622 KB)
- Español - ES (622 KB)
- Swedish - SV (622 KB)
- Italian - IT (622 KB)
- Portuguese - PT (622 KB)
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Handling Instructions (2659 KB)
References
[1]. Ma AY, et al. Nomegestrol Acetate Suppresses Human Endometrial Cancer RL95-2 Cells Proliferation In Vitro and In Vivo Possibly Related to Upregulating Expression of SUFU and Wnt7a. Int J Mol Sci. 2017 Jun 22;18(7):1337. [Content Brief]
[2]. van Diepen HA, et al. Nomegestrol acetate: steroid receptor transactivation profile in Chinese hamster ovary cells and ovulation inhibition in rat and monkey. Contraception. 2011 Aug;84(2):199-204. [Content Brief]
[3]. Mueck AO, et al. Nomegestrol acetate, a novel progestogen for oral contraception. Steroids. 2011 May;76(6):531-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6992 mL | 13.4960 mL | 26.9920 mL | 67.4800 mL |
| 5 mM | 0.5398 mL | 2.6992 mL | 5.3984 mL | 13.4960 mL | |
| 10 mM | 0.2699 mL | 1.3496 mL | 2.6992 mL | 6.7480 mL | |
| 15 mM | 0.1799 mL | 0.8997 mL | 1.7995 mL | 4.4987 mL | |
| 20 mM | 0.1350 mL | 0.6748 mL | 1.3496 mL | 3.3740 mL | |
| 25 mM | 0.1080 mL | 0.5398 mL | 1.0797 mL | 2.6992 mL | |
| 30 mM | 0.0900 mL | 0.4499 mL | 0.8997 mL | 2.2493 mL | |
| 40 mM | 0.0675 mL | 0.3374 mL | 0.6748 mL | 1.6870 mL | |
| 50 mM | 0.0540 mL | 0.2699 mL | 0.5398 mL | 1.3496 mL | |
| 60 mM | 0.0450 mL | 0.2249 mL | 0.4499 mL | 1.1247 mL | |
| 80 mM | 0.0337 mL | 0.1687 mL | 0.3374 mL | 0.8435 mL | |
| 100 mM | 0.0270 mL | 0.1350 mL | 0.2699 mL | 0.6748 mL |
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