MedChemExpress LLC (MCE)

MedChemExpress - Model Degarelix - 214766-78-6

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].

Degarelix

MCE China：Degarelix

Brand：MedChemExpress (MCE)

Cat. No.HY-16168A

CAS：214766-78-6

Synonyms：FE 200486 free base

Purity：99.94%

Storage：Sealed storage, away from moisture Powder -80°C 2 years -20°C 1 year *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

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.

In Vitro：Degarelix (FE 200486 free base) shows only very weak histamine-releasing properties and the lowest capacity for histamine release among the antagonists of LHRH, including Cetrorelix (HY-P0009), Abarelix (HY-13534), and Ganirelix (HY-P1628)[1]. Degarelix (1 nM-10 μM, 0-72 h) reduces cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1, VCaP cells), with the exception of the PC-3 cells[2]. Degarelix (10 μM, 0-72 h) exerts a direct effect on prostate cell growth through apoptosis[2].

In Vivo：Degarelix (FE 200486 free base) (0-10 μg/kg; s.c.; once) decreases plasma LH levels and plasma testosterone levels in a dose-dependent manner in castrated rats[3]. Degarelix (FE 200486 free base) is stable when incubated in microsomes and cryopreserved hepatocytes from animal liver tissue. In rat and dog, most of the degarelix dose is eliminated within 48 h via urine and feces in equal amounts (40–50% in each matrix), whereas in monkey the major route of excretion is fecal (50%) and renal (22%)[4].

IC50 & Target：GnRHR[1] Cellular Effect Cell Line Type Value Description References

References：

[1]. 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.

[2]. Degarelix.

[3]. 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. [Content Brief]

[4]. 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. [Content Brief]

[5]. 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. [Content Brief]

[6]. 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. [Content Brief]

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