Degarelix (acetate)

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Degarelix (acetate)

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Cat No: 24069

Biochemicals - Receptor Pharmacology

Degarelix is a synthetic gonadotropin-releasing hormone receptor (GNRHR) antagonist (IC50 = 3 nM in HEK293 cells expressing the human receptor).{39553} It inhibits the growth of WPMY-1, WPE1-NA22, BPH-1, and LNCaP prostate cell lines following a 72-ho...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-4-[[[(4S)-hexahydro-2,6-dioxo-4-pyrimidinyl]carbonyl]amino]-L-phenylalanyl-4-[(aminocarbonyl)amino]-D-phenylalanyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-D-alaninamide, monoacetate

Correlated keywords:

934246-14-7 214766-78-6 WPMY1 WPE1NA22 BPH1 HEK-293 R3327-H R-3327H 3327 FE200486 Gonax Firmagon 3327

Product Overview:
Degarelix is a synthetic gonadotropin-releasing hormone receptor (GNRHR) antagonist (IC50 = 3 nM in HEK293 cells expressing the human receptor).{39553} It inhibits the growth of WPMY-1, WPE1-NA22, BPH-1, and LNCaP prostate cell lines following a 72-hour incubation at a concentration of 10 μM via caspase activation and induction of apoptosis.{39554} In vivo, degarelix (2 mg/kg) decreases plasma testosterone levels in rats to castrate levels for the first 49 days post administration.{39553} It decreases tumor volume of Dunning R3327H prostate tumor flank implants in rats when administered at a dose of 1 mg/kg per month.{39555} Formulations containing degarelix have been used in the treatment of advanced prostate cancer.

Size	5 mg
Shipping	dry ice
CAS Number	934016-19-0
Molecular Formula	C₈₂H₁₀₃ClN₁₈O₁₆ • C₂H₄O₂
SMILES	O=C(N[C@H](CC1=CC=C(Cl)C=C1)C(N[C@H](CC2=CN=CC=C2)C(N[C@@H](CO)C(N[C@@H](CC3=CC=C(NC([C@@H]4CC(NC(N4)=O)=O)=O)C=C3)C(N[C@H](CC5=CC=C(NC(N)=O)C=C5)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCNC(C)C)C(N6[C@H](C(N[C@@H](C(N)=O)C)=O)CCC6)=O)=O)=O)=O)=O)=O)=O)[C@H](NC(C)=O
Molecular Weight	1692,3
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2924.19
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.