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Degarelix

Cat. No. M10250

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Degarelix Structure
Synonym:

FE-200486

Size Price Availability Quantity
1mg USD 60 In stock
5mg USD 160 In stock
10mg USD 270 In stock
25mg USD 440 In stock
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Quality Control & Documentation
Biological Activity

Degarelix 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.

Chemical Information
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
References

[1] Monica Sakai, et al. PLoS One. In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonist degarelix on human prostate cell growth

[2] Ferenc G Rick, et al. Onco Targets Ther. An update on the use of degarelix in the treatment of advanced hormone-dependent prostate cancer

[3] Anders Sonesson, et al. Drug Metab Dispos. Metabolite profiles of degarelix, a new gonadotropin-releasing hormone receptor antagonist, in rat, dog, and monkey

[4] Pierre Broqua, et al. J Pharmacol Exp Ther. Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormone antagonist: degarelix

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Keywords: Degarelix, FE-200486 supplier, LHRH/GnRH, inhibitors, activators

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