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GPCR/G Protein GNRH Receptor Degarelix

Degarelix

Catalog No. T10988   CAS 214766-78-6
Purity 98.00% Datasheet

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

Degarelix, CAS 214766-78-6
Pack Size Availability Price/USD Quantity
2 mg 3-7 days 102.00
5 mg 3-7 days 167.00
10 mg 3-7 days 275.00
50 mg 3-7 days 923.00
100 mg 3-7 days 1733.00
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Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
Targets&IC50 GnRHR,  
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.
Molecular Weight 1632.26
Formula C82H103ClN18O16
CAS No. 214766-78-6

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

H2O: 25 mg/mL (15.32 mM), Need ultrasonic

DMSO: 10 mg/mL (6.13 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References 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.

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Degarelix Danazol Relugolix Goserelin acetate Leuprorelin Leuprolide Acetate Elagolix sodium Cetrorelix

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