Degarelix acetate

• Catalog Number: orb2283077
• Category: Small Molecules
• Description: Degarelix acetate
• CAS Number: 934016-19-0
• MW: 1692.34
• 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
• Formula: C₈₄H₁₀₇ClN₁₈O₁₈
• Biological Activity: Degarelix is a synthetic gonadotropin-releasing hormone receptor (GNRHR) antagonist (IC50= 3 nM in HEK293 cells expressing the human receptor), effective in inhibiting the growth of various prostate cell lines (WPMY-1, WPE1-NA22, BPH-1, and LNCaP) by activating caspase and inducing apoptosis after 72 hours of exposure to 10 μM. In vivo studies demonstrate that degarelix (2 mg/kg) significantly reduces plasma testosterone levels in rats to castrate levels for up to 49 days following administration, and reduces the tumor volume of Dunning R3327H prostate tumor flank implants when given at a dose of 1 mg/kg per month. Formulations of degarelix are utilized in the treatment of advanced prostate cancer.
• Note: For research use only
• Expiration Date: 12 months from date of receipt.