Cat. No.: HY-16168B

Degarelix acetate hydrate

(Synonyms: FE 200486 acetate hydrate)

11 Cited Publications

Customer Review

Based on 11 publication(s) in Google Scholar

Degarelix acetate hydrate (FE 200486 acetate hydrate) is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research.

For research use only. We do not sell to patients.

CAS No.: 934246-14-7
Formula: C₈₂H₁₀₃ClN₁₈O₁₆.xC₂H₄O₂.xH₂O

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Degarelix acetate hydrate Chemical Structure

CAS No.: 934246-14-7

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

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

In Vitro

Degarelix 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)^[1].
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^[2].
Degarelix (10 μM, 0-72 h) exerts a direct effect on prostate cell growth through apoptosis^[2].

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

Cell Viability Assay^[2]

Cell Line:

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

1 nM-10 μM
Incubation Time:

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
Result:

Reduced cell viability in all prostate cell lines, with the exception of the PC-3 cells.

Apoptosis Analysis^[2]

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 (0-10 μg/kg; s.c.; once) decreases plasma LH levels and plasma testosterone levels in a dose-dependent manner in castrated rats^[3].
Degarelix 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%)^[4].

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

Animal Model:

Male Sprague-Dawley rats, castrated^[3]
Dosage:

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

Subcutaneous injection, once
Result:

Produced a dose-dependent and reversible decrease in plasma LH levels with a minimal effective dose of 3 μg/kg.
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 No. 934246-14-7
Formula C₈₂H₁₀₃ClN₁₈O₁₆.xC₂H₄O₂.xH₂O
Synonyms

FE 200486 acetate hydrate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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 hydrate 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 hydrate 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 hydrate 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 hydrate 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.
Microb Pathog

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

2024 Dec:197:107046. PMID: 39433139

Degarelix acetate hydrate 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 hydrate 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.
J Immunol

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

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 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)

References

[1]. 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]

[2]. 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]

[3]. 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]

[4]. 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]

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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.

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Degarelix acetate hydrate

11 Cited Publications

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Degarelix acetate hydrate

Publications Citing Use of MedChemExpress (MCE) Degarelix acetate hydrate

Biological Activity

Chemical Information

Publications (11)

Purity & Documentation

References

Calculators

Help & FAQs

Degarelix acetate hydrate Related Classifications

Cat. No.: HY-16168B