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Degarelix

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Catalog No. T10988Cas No. 214766-78-6
Alias FE200486 free base, FE 200486 free base

Degarelix is a peptide and selective GnRH (human gonadotropin-releasing hormone) receptor antagonist that treats prostate cancer by lowering testosterone levels in the body.

Degarelix

Degarelix

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Purity: 99.34%
Catalog No. T10988Alias FE200486 free base, FE 200486 free baseCas No. 214766-78-6
Degarelix is a peptide and selective GnRH (human gonadotropin-releasing hormone) receptor antagonist that treats prostate cancer by lowering testosterone levels in the body.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$185-In Stock
5 mg$516-In Stock
10 mg$825-In Stock
25 mg$1,4387-10 days7-10 days
50 mgInquiry7-10 days7-10 days
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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:99.34%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Degarelix is a peptide and selective GnRH (human gonadotropin-releasing hormone) receptor antagonist that treats prostate cancer by lowering testosterone levels in the body.
In vitro
Degarelix significantly reduced cell viability in multiple prostate-derived cell lines (1 nM–10 μM, 0–72 h), with no inhibitory effect on PC-3 cells[1].Degarelix suppressed prostate cell growth by inducing apoptosis (10 μM, 0–72 h)[1].
In vivo
In rats, a single subcutaneous dose of Degarelix (1–10 mg/kg, sc) caused dose-dependent testosterone suppression lasting >30 days[1].In prostate cancer patients, Degarelix (240 mg loading dose followed by monthly 80 mg sc) rapidly reduced serum testosterone to castrate levels (≤0.5 ng/mL), without the agonist-related hormone surge, and maintained suppression for at least 1 month[1].
SynonymsFE200486 free base, FE 200486 free base
Chemical Properties
Molecular Weight1632.26
FormulaC82H103ClN18O16
Cas No.214766-78-6
SmilesC([C@@H](NC([C@@H](NC([C@@H](CC1=CC=C(NC(N)=O)C=C1)NC([C@H](CC2=CC=C(NC(=O)[C@@H]3CC(=O)NC(=O)N3)C=C2)NC([C@@H](NC([C@@H](CC=4C=CC=NC4)NC([C@@H](CC5=CC=C(Cl)C=C5)NC([C@@H](CC6=CC7=C(C=C6)C=CC=C7)NC(C)=O)=O)=O)=O)CO)=O)=O)=O)CC(C)C)=O)CCCCNC(C)C)(=O)N8[C@H](C(N[C@@H](C(N)=O)C)=O)CCC8
Relative Density.1.325 g/cm3 (Predicted)
SequenceAc-D-2Nal-D-Phe(4-Cl)-D-3Pal-Ser-Phe(4-S-dihydroorotamido)-D-Phe(4-ureido)-Leu-Lys(iPr)-Pro-D-Ala-NH2
Sequence ShortXXXSXXLXPA
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: 4 mg/mL (2.45 mM), Sonication is recommended.
DMSO: 8 mg/mL (4.9 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (0.61 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
H2O/DMSO
1mg5mg10mg50mg
1 mM0.6126 mL3.0632 mL6.1265 mL30.6324 mL

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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:
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2 Enter the in vivo formulation:
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%
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