Degarelix (Synonyms: FE 200486 free base)

Name: Degarelix
Brand: MedChemExpress
SKU: HY-16168A
Rating: 5.0 (9 reviews)

Cat. No.: HY-16168A Purity: 99.92%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

Degarelix Chemical Structure

CAS No. : 214766-78-6

Size	Price	Stock	Quantity
2 mg	USD 108	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 670	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1050	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Degarelix:

9 Publications Citing Use of MCE Degarelix

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Biological Activity
Purity & Documentation
References
Customer Review

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]
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; ultrasonic and warming and heat to 60°C)

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:

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

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 (0.61 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (0.61 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1 mg/mL (0.61 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.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (255 KB) LCMS (412 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

9 Publications Citing Use of MCE Degarelix

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Degarelix Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Degarelix Related Classifications

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