Degarelix (Synonyms: FE 200486 free base)

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

Cat. No.: HY-16168A Purity: 99.96%: Data Sheet
COA

SDS
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 Degarelix acetate (FE 200486) is used for the research of prostate cancer.

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

Custom Peptide Synthesis

CAS No. : 214766-78-6

Size	Stock	Quantity
2 mg	In-stock	Estimated Time of Arrival: December 31
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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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Degarelix:

11 Publications Citing Use of MCE Degarelix

ELISA

In Vivo Efficacy Study

Cell Proliferation/Viability Assay

Histological Imaging/Staining

: Degarelix 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 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 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 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 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 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

IC₅₀ & Target

GnRHR^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.58 nM Compound: 1	Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay	[PMID: 16759096]
HEK293	IC₅₀	1.64 nM Compound: 2	Antagonism of GnRH response in HEK293 cells expressing human GnRH receptor Antagonism of GnRH response in HEK293 cells expressing human GnRH receptor	[PMID: 16033265]
HEK293	IC₅₀	8.8 nM Compound: 32	Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells	[PMID: 11462984]
Mast cell	EC₅₀	> 1000 μg/mL Compound: 1	Histamine release in mast cells by ELISA Histamine release in mast cells by ELISA	[PMID: 16759096]

In Vitro

Degarelix (FE 200486 free base) 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 (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^[3].
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%)^[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.

Clinical Trial

Molecular Weight

1632.26

Formula

C₈₂H₁₀₃ClN₁₈O₁₆

CAS No.

214766-78-6

Appearance

Solid

Color

White to off-white

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, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (6.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 5 mg/mL (3.06 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.6126 mL	3.0632 mL	6.1265 mL
5 mM	0.1225 mL	0.6126 mL	1.2253 mL
10 mM	---	---	---

View the Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 12.5 mg/mL (7.66 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (283 KB) SDS (396 KB)

COA (255 KB) RP-HPLC (246 KB) MS (239 KB) Elemental Analysis Report (113 KB)

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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	0.6126 mL	3.0632 mL	6.1265 mL	15.3162 mL
DMSO	5 mM	0.1225 mL	0.6126 mL	1.2253 mL	3.0632 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.

Degarelix Related Classifications

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:

Degarelix214766-78-6FE 200486FE200486FE-200486GnRH ReceptorApoptosisGonadotropin releasing hormone receptorGNRHRprostate cancerLHRHluteinizing hormone-releasing hormoneInhibitorinhibitorinhibit

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Degarelix (Synonyms: FE 200486 free base)

Customer Review

Other Forms of Degarelix:

Degarelix Related Antibodies

11 Publications Citing Use of MCE Degarelix

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Biological Activity

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References

Customer Review

Degarelix Related Antibodies

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Complete Stock Solution Preparation Table

Degarelix Related Classifications

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