2. GPCR/G Protein Apoptosis
  3. GnRH Receptor Apoptosis
  4. 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
5 mg USD 180 In-stock
10 mg USD 300 In-stock
50 mg USD 1020 In-stock
100 mg USD 1920 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Degarelix:

Degarelix Related Antibodies

Top Publications Citing Use of Products

  • 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].

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

Degarelix Related Antibodies

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].

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, 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

Appearance

Solid

Formula

C82H103ClN18O16
CAS No.
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)

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 MedChemExpress (MCE).
Purity & Documentation

Purity: 99.92%

COA (255 KB) LCMS (412 KB) Elemental Analysis Report (113 KB)

Handling Instructions (2659 KB)
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.

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.

  • 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

Keywords:

Degarelix214766-78-6GnRH ReceptorApoptosisGonadotropin releasing hormone receptorGNRHRprostate cancerLHRHluteinizing hormone-releasing hormoneInhibitorinhibitorinhibit

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:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.