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Degarelix

Catalog No. T10988   CAS 214766-78-6

Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.

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Degarelix Chemical Structure
Degarelix, CAS 214766-78-6
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50 mg 5 days $ 847.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
In vitro 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.
In vivo In a single subcutaneous injection of 0.3 to 10 μg/kg in rats, degarelix produced a dose-dependent inhibition of the pituitary-gonad axis as revealed by the decrease in plasma luteinizing hormone (LH) and testosterone levels. The duration of LH inhibition increased with increasing dose: in rats, after subcutaneous injection of digarelix 12.5, 50 or 200 μg/kg, the significant inhibition of LH lasted 1, 2 and 7 days, respectively [ 3]. Degarelix is stable when incubated in microsomes and liver cells cryopreserved in animal liver tissue.
Molecular Weight 1632.26
Formula C82H103ClN18O16
CAS No. 214766-78-6

Storage

keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 25 mg/mL (15.32 mM), Sonication is recommended.

DMSO: 10 mg/mL (6.13 mM), Sonication is recommended.

TargetMolReferences and Literature

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.

Related Products

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(R)-Elagolix Cetrorelix Acetate Abarelix Deslorelin acetate(57773-65-6 free base) Elagolix sodium Degarelix acetate(214766-78-6 free base) Ganirelix Acetate LGnRH-III, lamprey acetate(147859-97-0 free base)

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Keywords

Degarelix 214766-78-6 GPCR/G Protein GNRH Receptor inhibitor inhibit

 

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