1. GPCR/G Protein
  2. GNRH Receptor
  3. Degarelix


Cat. No.: HY-16168A Purity: 99.92%
Handling Instructions

Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.

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

Degarelix Chemical Structure

Degarelix Chemical Structure

CAS No. : 214766-78-6

Size Price Stock Quantity
10 mM * 1 mL in Water USD 539 In-stock
Estimated Time of Arrival: December 31
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 1020 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1920 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review


Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.

IC50 & Target


In Vitro

Degarelix acts directly on the pituitary receptors for luteinizing hormone-releasing hormone (LHRH), blocking the action of endogenous LHRH. The use of degarelix eliminates the initial undesirable surge in gonadotropin and testosterone levels, which is produced by agonists of LHRH[1]. Degarelix treatment reduces cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1 cells, VCaP cells), with the exception of the PC-3 cells. The GnRH antagonist degarelix exerts a direct effect on prostate cell growth through apoptosis[2].

In Vivo

At single subcutaneous injections of 0.3 to 10 μg/kg in rats, degarelix produces a dose-dependent suppression of the pituitary-gonadal axis as revealed by the decrease in plasma luteinizing hormone (LH) and testosterone levels. Duration of LH suppression increases with the dose: in the rat, significant suppression of LH lasted 1, 2, and 7 days after a single subcutaneous injection of degarelix at 12.5, 50, or 200 μg/kg, respectively[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].

Clinical Trial
Molecular Weight







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


Room temperature in continental US; may vary elsewhere

Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : ≥ 500 mg/mL (306.32 mM)

*"≥" means soluble, but saturation unknown.

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 0.0613 mL 0.3063 mL 0.6126 mL
*Please refer to the solubility information to select the appropriate solvent.
Cell Assay

Cells are allowed to attach for 24–48 hours (h). After that, they are treated with different concentrations of degarelix, a GnRH antagonist (0.1 to 10 μM). 10 μL of MTT labeling reagent is added to each well and the plates are incubated at 37°C for 4h. Then, 100 μL of solubilization solution is added, and the plates are incubated at 37°C, overnight, in a humidified atmosphere. The final reaction is measured at 550–600 nm. The obtained absorbance directly correlates to the number of live and metabolically active cells, providing an indication of cell viability[2].

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

Animal Administration

Rats: To study the absorption, distribution, metabolism, and excretion, male and female rats are dosed with 30 μg [3H]degarelix free base peptide/kg (-300 μCi/kg). Feces, heparin plasma, and urine samples from groups A and B are collected up to 240 h after dosing. Bile sampling from cannulated rats (group C) as well as urine and feces are collected for up to 48 h. All samples in this study are analyzed by LC-RAD at the contract research[4].

Monkeys: Four male cynomolgus Monkeys (4.2-7.5 kg) are dosed for a disposition of radioactivity study. The animals are administered a single subcutaneous dose of 8.2 μg/kg (200 μCi/kg) [3H]degarelix. Urine and feces samples are collected quantitatively from each animal after dosing until the time of sacrifice. Blood samples are collected at the time of the sacrifice of the individual animal (6, 24, 48, and 240 h) into tubes containing EDTA as an anticoagulant[4].

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


Purity: 99.92%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name



Applicant name *


Email address *

Phone number *


Organization name *

Country or Region *


Requested quantity *


Bulk Inquiry

Inquiry Information

Product Name:
Cat. No.: