1. GPCR/G Protein
    Apoptosis
  2. GnRH Receptor
    Apoptosis
  3. Degarelix

Degarelix 

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

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

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

Custom Peptide Synthesis

Degarelix Chemical Structure

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 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

Other Forms of Degarelix:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Degarelix

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix can be used for prostate cancer research[1].

IC50 & Target

GnRHR[1]

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].

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].

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, t1/2 of absorption values were 4 min and 30 min, Tmax values were 1 h and 5 h, and apparent plasma disappearance t1/2 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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (6.13 mM; Need ultrasonic)

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 --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (0.61 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.92%

References
  • 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.
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.

  • 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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Degarelix
Cat. No.:
HY-16168A
Quantity:
MCE Japan Authorized Agent: