Art. -Nr.: HY-16168

Degarelix acetate

Name: Degarelix acetate
Brand: MedChemExpress
SKU: HY-16168
Price: 180.00 USD
Availability: InStock
Rating: 5 (11 reviews)

(Synonyms: FE 200486)

11 Cited Publications

Kundenbewertung

Based on 11 publication(s) in Google Scholar

Degarelix acetate (FE 200486) is a decapeptide that shows high affinity/selectivity to human gonadotropin-releasing hormone (GnRH) receptor (IC₅₀ = 3 nM). Degarelix acetate (FE 200486) is used for the research of prostate cancer.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.67%
CAS. Nr.: 934016-19-0
Formel: C₈₄H₁₀₇ClN₁₈O₁₈
Molecular Weight:1692.31

Speicherung:

Sealed storage, away from moisture.

Powder -80°C, 2 years , -20°C, 1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Degarelix acetate Chemical Structure

CAS. Nr.: 934016-19-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (1)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

Degarelix (FE 200486) shows only very weak histamine-releasing properties and the lowest capacity for histamine release among the antagonists of LHRH, including Cetrorelix (HY-P0009), Abarelix (HY-13534), and Ganirelix (HY-P1628)^[3].
Degarelix (1 nM-10 μM, 0-72 h) reduces cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1, VCaP cells), with the exception of the PC-3 cells^[4].
Degarelix (10 μM, 0-72 h) exerts a direct effect on prostate cell growth through apoptosis^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Cell Viability Assay^[4]

View Protocol

Cell Line:

WPMY-1, WPE1-NA22, BPH-1, LNCaP and VCaP.
Concentration:

1 nM-10 μM.
Incubation Time:

48-72 h
Result:

WPMY-1 cells at 48 and 72h, WPE1-NA22 cells at 72 hours, BPH-1 cells at 48 and 72h, LNCaP cells at 48 and 72h. Reduced cell viability in all prostate cell lines, with the exception of the PC-3 cells.

Apoptosis Analysis^[4]

View Protocol

Cell Line:

WPE1-NA22, BPH-1, LNCaP and VCaP.
Concentration:

10 μM.
Incubation Time:

24, 48 and 72 h.
Result:

Induced a significant increase on caspase 3/7 activation.

In Vivo

Degarelix (FE 200486 free base) (0-10 μg/kg; s.c.; once) decreases plasma LH levels and plasma testosterone levels in a dose-dependent manner in castrated rats^[5].
Degarelix (FE 200486 free base) is stable when incubated in microsomes and cryopreserved hepatocytes from animal liver tissue. In rat and dog, most of the degarelix dose is eliminated within 48 h via urine and feces in equal amounts (40-50% in each matrix), whereas in monkey the major route of excretion is fecal (50%) and renal (22%)^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male Sprague-Dawley rats, castrated^[5].
Dosage:

0.3, 1, 3 and 10 μg/kg or 12.5, 50, and 200 μg/kg.
Administration:

Subcutaneous injection, once.
Result:

For the 50 μg/kg and 200 μg/kg doses, t_1/2 of absorption values were 4 min and 30 min, T_max values were 1 h and 5 h, and apparent plasma disappearance t_1/2 values were 12 h and 67 h, respectively.
Produced a dose-dependent decrease in plasma testosterone levels with a minimal effective dose of 1 μg/kg.

Chemical Information

CAS. Nr. 934016-19-0
Appearance Solid
Molecular Weight 1692.31
Formel C₈₄H₁₀₇ClN₁₈O₁₈
Color White to off-white
SMILES

C[C@H](C(N)=O)NC([C@H]1N(C([C@H](CCCCNC(C)C)NC([C@H](CC(C)C)NC([C@@H](CC2=CC=C(NC(N)=O)C=C2)NC([C@H](CC3=CC=C(NC([C@H](CC(N4)=O)NC4=O)=O)C=C3)NC([C@H](CO)NC([C@@H](CC5=CC=CN=C5)NC([C@@H](CC6=CC=C(Cl)C=C6)NC([C@@H](CC7=CC=C8C=CC=CC8=C7)NC(C)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC1)=O.O=C(O)C
Synonyms

FE 200486
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (11)

All ELISAIn Vivo Efficacy StudyCell Proliferation/Viability AssayHistological Imaging/Staining

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Journal Impact Factor

Nat Cell Biol

An extracellular vesicle-mediated mitochondrial transfer network critical for testosterone synthesis. [Abstract]

2026 Apr;28(4):707-724. PMID: 41760931
Cancer Lett

SOX2 expression in prostate cancer drives resistance to nuclear hormone receptor signaling inhibition through the WEE1/CDK1 signaling axis. [Abstract]

2023 Jul 1:565:216209. PMID: 37169162
Arterioscler Thromb Vasc Biol

FSH Is Responsible for Androgen Deprivation Therapy-Associated Atherosclerosis in Mice by Exaggerating Endothelial Inflammation and Monocyte Adhesion. [Abstract]

2024 Mar;44(3):698-719. PMID: 38205641

Degarelix acetate purchased from MedChemExpress. Usage Cited in: Arterioscler Thromb Vasc Biol. 2024 Mar;44(3):698-719. [Abstract]

Serum levels of testosterone and follicle-stimulating hormone (FSH) in mice were assessed by ELISA. Degarelix (Deg) (50 mg/kg; s.c.; once a month) rapidly reduced FSH and testosterone levels in high-fat diet–fed male ApoE^−/− mice.

Degarelix acetate purchased from MedChemExpress. Usage Cited in: Arterioscler Thromb Vasc Biol. 2024 Mar;44(3):698-719. [Abstract]

The Degarelix (Deg) (50 mg/kg; s.c.; once a month) group showed similar or even smaller atherosclerotic lesions in the aortic root and aortic tree of high-fat diet–fed male ApoE^−/− mice compared with the saline group.

Degarelix acetate purchased from MedChemExpress. Usage Cited in: Arterioscler Thromb Vasc Biol. 2024 Mar;44(3):698-719. [Abstract]

SmαA (smooth muscle α-actin) and F4/80 immunostaining (red) on the plaques of aortic roots of mice. Degarelix (Deg) (50 mg/kg; s.c.; once a month) barely changed macrophage contents, smooth muscle cells and collagen contents.
FASEB J

Circadian disruption impairs glucose homeostasis in male but not in female mice and is dependent on gonadal sex hormones. [Abstract]

2023 Feb;37(2):e22772. PMID: 36645117

Degarelix acetate purchased from MedChemExpress. Usage Cited in: FASEB J. 2023 Feb;37(2):e22772. [Abstract]

Degarelix (25 mg/kg; s.c.; at days 1 and 29) decreased seminal vesicle and ovary weight, suppressed gonadal sex hormone production, and reduced rhythm strength and total food intake in male and female C57BL/6J mice.
J Immunol

Restored Thymic Output after Androgen Blockade Participates in Antitumor Immunity. [Abstract]

2023 Feb 15;210(4):496-503. PMID: 36548468
Microb Pathog

Degarelix limits the survival of mycobacteria and granuloma formation. [Abstract]

2024 Dec:197:107046. PMID: 39433139

Degarelix acetate purchased from MedChemExpress. Usage Cited in: Microb Pathog. 2024 Dec:197:107046. [Abstract]

Degarelix (10 mg/kg; p.o.; once daily for 14 d) supplementation led to a lower bacterial burden and less granuloma formation in zebrafish adults infected with M. marinum compared to those fish treated with mock, while degarelix therapeutic effects were similar to RFP effects.

Degarelix acetate purchased from MedChemExpress. Usage Cited in: Microb Pathog. 2024 Dec:197:107046. [Abstract]

BMDMs pretreated with degarelix (1 μM), aminoguanidine hydrochloride (AGHS, 100 μM), BafA1 (100 nM), NAC (5 mM), Z-VAD (20 μM), or 3-MA (5 mM) were infected with H37Rv (MOI = 2). At different time points after infection, bacterial survival was calculated by dividing the CFU at 24 h by the CFU at 3 h.
Prostate

Gonadotropin-releasing hormone antagonist associated with lower cardiovascular risk compared with gonadotropin-releasing hormone agonist in prostate cancer: A nationwide cohort and in vitro study. [Abstract]

2021 Sep;81(12):902-912. PMID: 34196430
Res Sq

2025 Apr 07.
SSRN

2024 May 22.
bioRxiv

Suppression of tumor cell lactate-generating signaling pathways eradicates murine PTEN/p53-deficient aggressive-variant prostate cancer via macrophage phagocytosis. [Abstract]

2023 May 23:2023.05.23.540590. PMID: 37292972
Research Square Preprint

2020 Mar 27.

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : 20 mg/mL (11.82 mM; Need ultrasonic)

DMSO : 10 mg/mL (5.91 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.5909 mL

2.9545 mL

5.9091 mL

5 mM

0.1182 mL

0.5909 mL

1.1818 mL

10 mM

0.0591 mL

0.2955 mL

0.5909 mL

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 1 mg/mL (0.59 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 1 mg/mL (0.59 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1 mg/mL (0.59 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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) .

Protokoll

All Signal Pathway Related

Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Anders Sonesson, et al. In Vitro and In Vivo Human Metabolism of Degarelix, a Gonadotropin-Releasing Hormone Receptor Blocker. Drug Metabolism and Disposition. July 2013, 41 (7) 1339-1346.

[2]. Degarelix.

[3]. Rick FG, et al. An update on the use of degarelix in the treatment of advanced hormone-dependent prostate cancer. Onco Targets Ther. 2013 Apr 16;6:391-402. [Content Brief]

[4]. Sakai M, et al. In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonistdegarelix on human prostate cell growth. PLoS One. 2015 Mar 26;10(3):e0120670. [Content Brief]

[5]. Broqua P, et al. Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormoneantagonist: degarelix. J Pharmacol Exp Ther. 2002 Apr;301(1):95-102. [Content Brief]

[6]. Sonesson A, et al. Metabolite profiles of degarelix, a new gonadotropin-releasing hormone receptor antagonist, in rat, dog, and monkey. Drug Metab Dispos. 2011 Oct;39(10):1895-903. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	0.5909 mL	2.9545 mL	5.9091 mL	14.7727 mL
DMSO / H₂O	5 mM	0.1182 mL	0.5909 mL	1.1818 mL	2.9545 mL
H₂O	10 mM	0.0591 mL	0.2955 mL	0.5909 mL	1.4773 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Bioz

Keywords

Degarelix acetate

11 Cited Publications

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Degarelix acetate

Publications Citing Use of MedChemExpress (MCE) Degarelix acetate