1. Vitamin D Related/Nuclear Receptor
  2. Progesterone Receptor
  3. Nomegestrol acetate

Nomegestrol acetate  (Synonyms: ノメゲストロール アセタート)

製品番号: HY-105634A 純度: 99.73%
COA 取扱説明書 Technical Support

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.

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Nomegestrol acetate

Nomegestrol acetate 構造式

CAS 番号 : 58652-20-3

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 62 在庫あり
Solution
10 mM * 1 mL in DMSO USD 62 在庫あり
Solid
5 mg $57 在庫あり
10 mg $90 在庫あり
25 mg $174 在庫あり
50 mg $272 在庫あり
100 mg $410 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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製品説明

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[1][2][3].

IC50 & Target

Progesterone receptor[3].

体外実験

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.

Cell Proliferation Assay[1]

Cell Line: RL95-2 cells
Concentration: 0.3, 1, 3, 10, 30, and 100 µM
Incubation Time: 24, 48, 72 h
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.

Western Blot Analysis[1]

Cell Line: RL95-2 cells
Concentration: 4, 20, 100 µM
Incubation Time: 6, 24, 48 h
Result: Increased the protein levels of SUFU and Wnt7a (relative to GAPDH expression) in a concentration-dependent manner.
体内実験

Nomegestrol acetate (50, 100, 200 mg/kg; p.o.; single daily for 28 days) inhibits growth of RL95-2 xenograft tumors in vivo[1].
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.

Animal Model: Female athymic nude mice (BALB/c; 18-20 g; 6 to 7-week-old; xenograft nude mouse model)[1].
Dosage: 50, 100, 200 mg/kg
Administration: Oral gavage; single daily for 28 days
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.
Animal Model: Mature female Wistar rats (~200 g)[2].
Dosage: 1, 2.5 mg/rat
Administration: Oral administration; single daily for 4 days
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.
臨床実験
分子量

370.48

分子式

C23H30O4

CAS 番号
Appearance

Solid

Color

White to off-white

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6992 mL 13.4960 mL 26.9920 mL
5 mM 0.5398 mL 2.6992 mL 5.3984 mL
10 mM 0.2699 mL 1.3496 mL 2.6992 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

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体積 (開始)

V1

=
濃度 (終了)

C2

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体積 (終了)

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体内:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション

純度: 99.73%

参考文献

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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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
Nomegestrol acetate
製品番号:
HY-105634A
数量:
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