Degarelix

SKU: orb1709906

Description

Degarelix is a synthetic peptide antagonist of the gonadotropin-releasing hormone (GnRH) receptor. It is utilized in prostate cancer research to rapidly suppress testosterone production, facilitating studies on androgen deprivation in both in vitro cellular models and in vivo xenograft experiments.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 214766-78-6
• MW: 1632.26
• Purity: 99.34%
• Formula: C₈₂H₁₀₃ClN₁₈O₁₆
• SMILES: C([C@@H](NC([C@@H](NC([C@@H](CC1=CC=C(NC(N)=O)C=C1)NC([C@H](CC2=CC=C(NC(=O)[C@@H]3CC(=O)NC(=O)N3)C=C2)NC([C@@H](NC([C@@H](CC=4C=CC=NC4)NC([C@@H](CC5=CC=C(Cl)C=C5)NC([C@@H](CC6=CC7=C(C=C6)C=CC=C7)NC(C)=O)=O)=O)=O)CO)=O)=O)=O)CC(C)C)=O)CCCCNC(C)C)(=O)N8[C@H](C(N[C@@H](C(N)=O)C)=O)CCC8
• Target: Apoptosis,GNRH Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (0.61 mM);H2O:4 mg/mL (2.45 mM);DMSO:8 mg/mL (4.9 mM)

Bioactivity

• In Vivo:
  In rats, a single subcutaneous dose of Degarelix (1–10 mg/kg, sc) caused dose-dependent testosterone suppression lasting >30 days.In prostate cancer patients, Degarelix (240 mg loading dose followed by monthly 80 mg sc) rapidly reduced serum testosterone to castrate levels (≤0.5 ng/mL), without the agonist-related hormone surge, and maintained suppression for at least 1 month.
• In Vitro:
  Degarelix significantly reduced cell viability in multiple prostate-derived cell lines (1 nM–10 μM, 0–72 h), with no inhibitory effect on PC-3 cells.Degarelix suppressed prostate cell growth by inducing apoptosis (10 μM, 0–72 h).

Storage & Handling

• Storage: keep away from moisture | store at -20°C | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GNRH Receptor, GnRHR, GNRHReceptor, FE200486 free base, FE 200486 free base, Degarelix

Compound Identifiers

PubChem CID

16136245