Degarelix acetate(214766-78-6 free base)

SKU: orb1309779

Description

Degarelix acetate is a synthetic peptide antagonist that competitively and reversibly inhibits the gonadotropin-releasing hormone receptor (GnRHR). It is widely used in research applications, including in vitro binding assays and in vivo models for studying hormone-dependent conditions such as prostate cancer.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 934016-19-0
• MW: 1692.34
• Purity: 98.66% (May vary between batches)
• Formula: C₈₄H₁₀₇ClN₁₈O₁₈
• SMILES: CC(O)=O.CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O
• Target: GNRH Receptor
• Solubility: DMSO:16.93 mg/mL (10 mM)

Bioactivity

• In Vivo:
  In a single subcutaneous injection of 0.3 to 10 μg/kg in rats, degarelix produced a dose-dependent inhibition of the pituitary-gonad axis as revealed by the decrease in plasma luteinizing hormone (LH) and testosterone levels. The duration of LH inhibition increased with increasing dose: in rats, after subcutaneous injection of digarelix 12.5, 50 or 200 μg/kg, the significant inhibition of LH lasted 1, 2 and 7 days, respectively [ 3]. Degarelix is stable when incubated in microsomes and liver cells cryopreserved in animal liver tissue.
• In Vitro:
  Degarelix directly acts on the pituitary receptors to luteinizing hormone-releasing hormone (LHRH), preventing the effect of endogenous LHRH. The use of degarelix eliminates the undesirable surge of initial gonadotropin and testosterone levels produced by LHRH agonists. With the exception of PC-3 cells, Degarelix treatment reduces the cell viability of all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1 cells, VCaP cells). GnRH antagonist degarelix has a direct effect on the growth of prostate cells through apoptosis.

Storage & Handling

• Storage: keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Degarelix acetate(214766 78 6 free base), Degarelix acetate(214766786 free base), Degarelix acetate(214766-78-6 free base), GNRHReceptor, GnRHR, GNRH Receptor

Compound Identifiers

PubChem CID

16186010