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Degarelix

CAT: 0804-HY-16168A-01Size: 2 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-16168A-01Size:2 mg
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Description
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].
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.
Shipping Conditions
Blue Ice
Storage Conditions
-80°C, 2 years; -20°C, 1 year (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Launched