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Degarelix (GSK1278863) is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist. 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. Degarelix (0.3 to 10 μg/kg) in rats produces a dose-dependent suppression of the pituitary-gonadal axis as revealed by the decrease in plasma luteinizing hormone (LH) and testosterone levels.
| Molecular Weight | 1632.26 |
| Formula | C82H103ClN18O16 |
| CAS Number | 214766-78-6 |
| Solubility (25°C) | DMSO 10 mg/mL Water 5 mg/mL (ultrasonic and warming) |
| Storage | -20°C, dry, sealed |
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