Degarelix acetate (Synonyms: FE 200486)

Name: Degarelix acetate
Brand: MedChemExpress
SKU: HY-16168
Rating: 5.0 (11 reviews)

Cat. No.: HY-16168: Data Sheet Handling Instructions
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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.

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

CAS No. : 934016-19-0

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 11 publication(s) in Google Scholar

Other Forms of Degarelix acetate:

Degarelix In-stock
Degarelix-d₇ Get quote
Degarelix acetate hydrate Get quote

11 Publications Citing Use of MCE Degarelix acetate

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In Vivo Efficacy Study

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Histological Imaging/Staining

: 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.

: 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.

: 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.

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Description

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.

Cell Viability Assay^[4]

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]

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.

Molecular Weight

1692.31

Formula

C₈₄H₁₀₇ClN₁₈O₁₈

CAS No.

934016-19-0

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

Degarelix acetate Related Classifications

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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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.

Keywords:

Degarelix934016-19-0FE 200486FE200486FE-200486GnRH ReceptorGonadotropin releasing hormone receptorGNRHRgonadotropin-releasing hormoneGnRHprostate cancerInhibitorinhibitorinhibit

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Degarelix acetate (Synonyms: FE 200486)

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Other Forms of Degarelix acetate:

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11 Publications Citing Use of MCE Degarelix acetate

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