Degarelix

Degarelix acetate (FE 200486) is a decapeptide that shows high affinity/selectivity to human gonadotropin-releasing hormone (GnRH) receptor (IC50 = 3 nM) . Degarelix acetate Degarelix acetate (FE 200486) is used for the research of prostate cancer[1][2].

Product Specifications

CAS Number

[214766-78-6]

Product Name Alternative

FE 200486 (free base)

UNSPSC

12352209

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; GnRH Receptor

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein

Applications

Cancer-programmed cell death

Field of Research

Cancer; Endocrinology

Assay Protocol

https://www.medchemexpress.com/Degarelix.html

Purity

99.96

Solubility

DMSO : 10 mg/mL (ultrasonic) |H2O : 5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

C[C@H](C(N)=O)NC([C@H]1N(C([C@H](CCCCNC(C)C)NC([C@H](CC(C)C)NC([C@@H](CC2=CC=C(NC(N)=O)C=C2)NC([C@H](CC3=CC=C(NC([C@H](CC(N4)=O)NC4=O)=O)C=C3)NC([C@H](CO)NC([C@@H](CC5=CC=CN=C5)NC([C@@H](CC6=CC=C(Cl)C=C6)NC([C@@H](CC7=CC=C8C=CC=CC8=C7)NC(C)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC1)=O

Molecular Formula

C82H103ClN18O16

Molecular Weight

1632.26

Precautions

H302, H315, H319, H335

References & Citations

[1]Rick FG, et al. An update on the use of degarelix in the treatment of advanced hormone-dependent prostate cancer. Onco Targets Ther. 2013 Apr 16;6:391-402.|[2]Sakai M, et al. In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonistdegarelix on human prostate cell growth. PLoS One. 2015 Mar 26;10 (3) :e0120670.|[3]Broqua P, et al. Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormoneantagonist: degarelix. J Pharmacol Exp Ther. 2002 Apr;301 (1) :95-102.|[4]Sonesson A, et al. Metabolite profiles of degarelix, a new gonadotropin-releasing hormone receptor antagonist, in rat, dog, and monkey. Drug Metab Dispos. 2011 Oct;39 (10) :1895-903.|[5]Anders Sonesson, et al. In Vitro and In Vivo Human Metabolism of Degarelix, a Gonadotropin-Releasing Hormone Receptor Blocker. Drug Metabolism and Disposition. July 2013, 41 (7) 1339-1346.|[6]Degarelix.