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Nestoron

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Catalog No. T5174Cas No. 7759-35-5
Alias ST-1435, Segesterone Acetate, Nestorone, Elcometrine

Nestoron (Segesterone Acetate), a synthetic progestin, is a high-affinity agonist of the progesterone receptor (EC50: 10.3 nM).

Nestoron

Nestoron

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Purity: 99.92%
Catalog No. T5174Alias ST-1435, Segesterone Acetate, Nestorone, ElcometrineCas No. 7759-35-5
Nestoron (Segesterone Acetate), a synthetic progestin, is a high-affinity agonist of the progesterone receptor (EC50: 10.3 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$35In StockIn Stock
10 mg$57In StockIn Stock
25 mg$118In StockIn Stock
50 mg$226In StockIn Stock
100 mg$365In StockIn Stock
1 mL x 10 mM (in DMSO)$63In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.92%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
Nestoron (Segesterone Acetate), a synthetic progestin, is a high-affinity agonist of the progesterone receptor (EC50: 10.3 nM).
Targets&IC50
PR:10.3 nM
In vitro
Nestorone (ST-1435) showed significant binding (ED50 = 56 nM) compared to the binding of dexamethasone (ED50 = 21 nM) to calf thymus GR. Progesterone and Nestorone showed no binding to SHBG [1]. Chronic ST-1435 and E2 alone or in combination increased neurogenesis by a comparable magnitude, with minimum to no antagonistic or additive effects between ST-1435 and E2. In addition, chronic exposure of ST-1435 or ST-1435 + E2 stimulated oligodendrocyte generation [2].
In vivo
The potency of Nestorone was over 100-fold higher upon s.c. administration than via the oral route. Nestorone showed no androgenic or anabolic activity. Nestorone did not bind to sex hormone binding globulin (SHBG). In contrast to estradiol and levonorgestrel, Nestorone showed no uterotropic activity in ovariectomized rats. Despite significant binding to glucocorticoid receptors (GR), Nestorone showed no glucocorticoid activity in vivo [1].
Animal Research
Immature female rats were ovariectomized under methoxylflurane anesthesia, randomly distributed into treatment groups (n 5 6 per group), and used 5 to 7 days later. Levonorgestrel or Nestorone (1 or 5 mg) was injected s.c. daily for 5 days. Vaginal lavages were examined microscopically to detect vaginal cornification. The animals were killed on day 6, and the uteri were removed, cleaned, blotted dry, and weighed. The antiestrogenic effects of levonorgestrel and Nestorone were determined in rats receiving 1.0 mg E2. A positive control group received E2 alone. Negative controls received the vehicle [1].
SynonymsST-1435, Segesterone Acetate, Nestorone, Elcometrine
Chemical Properties
Molecular Weight370.48
FormulaC23H30O4
Cas No.7759-35-5
Smiles[H][C@@]12CC(=C)[C@](OC(C)=O)(C(C)=O)[C@@]1(C)CC[C@]1([H])[C@@]3([H])CCC(=O)C=C3CC[C@@]21[H]
Relative Density.1.0550 g/cm3 (Estimated)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 55 mg/mL (148.46 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.4 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6992 mL13.4960 mL26.9920 mL134.9601 mL
5 mM0.5398 mL2.6992 mL5.3984 mL26.9920 mL
10 mM0.2699 mL1.3496 mL2.6992 mL13.4960 mL
20 mM0.1350 mL0.6748 mL1.3496 mL6.7480 mL
50 mM0.0540 mL0.2699 mL0.5398 mL2.6992 mL
100 mM0.0270 mL0.1350 mL0.2699 mL1.3496 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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