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Degarelix acetate(214766-78-6 free base)

Catalog No. T10988L CAS T10988L

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

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Degarelix acetate(214766-78-6 free base) Chemical Structure

Degarelix acetate(214766-78-6 free base), CAS T10988L

Pack Size	Availability	Price/USD
1 mg	In stock	$ 70.00
2 mg	In stock	$ 100.00
5 mg	In stock	$ 168.00
10 mg	In stock	$ 280.00
25 mg	In stock	$ 503.00
50 mg	In stock	$ 732.00
100 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 513.00

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Purity: 98.66%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Degarelix acetate is a competitive and reversible antagonist of gonadotropin-releasing hormone receptor (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.
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	1692.34
Formula	C84H107ClN18O18
CAS No.	T10988L

Storage

keep away from moisture

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

Solubility Information

DMSO: 16.92 mg/mL (10 mM)

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.

Related compound libraries

This product is contained In the following compound libraries：

Peptide Compound Library NO PAINS Compound Library GPCR Compound Library Inhibitor Library FDA-Approved & Pharmacopeia Drug Library Anti-Prostate Cancer Compound Library

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AG 045572 LHRH Cetrorelix Acetate Abarelix Deslorelin acetate(57773-65-6 free base) Linzagolix GnRH-R antagonist 1 Histrelin acetate

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Keywords

Degarelix acetate(214766-78-6 free base) T10988L GPCR/G Protein GNRH Receptor Degarelix acetate(214766786 free base) Degarelix acetate(214766 78 6 free base) inhibitor inhibit

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