Degarelix acetate hydrate
Degarelix acetate hydrate (FE 200486 acetate hydrate) is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research.
For research use only. We do not sell to patients.
- CAS No.: 934246-14-7
- Formula: C82H103ClN18O16.xC2H4O2.xH2O
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-16168A
DegarelixGnRHR Antagonist -
HY-16474
RelugolixGnRH Antagonist -
HY-P0013
AntideLHRH Antagonist -
HY-14789
(R)-ElagolixGnRH Receptor Antagonist -
HY-13534
AbarelixGnRH Antagonist -
HY-16168
Degarelix acetateGnRH Anagonist -
HY-16532
Zoptarelin doxorubicinHybrid Anticancer Agent -
HY-P1808
LGnRH-III, lampreyGnRH Agonist -
HY-P3582
sGnRH-AGnRH Analogue -
HY-134864
LumigolixGnRH Receptor Antagonist -
HY-16474R
Relugolix (Standard)GnRH Antagonist -
HY-14789R
(R)-Elagolix (Standard)GnRH Receptor Antagonist
Biological Activity
Description
In Vitro
Degarelix 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:WPMY-1, WPE1-NA22, BPH-1, LNCaP and VCaP
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Concentration:1 nM-10 μM
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Incubation Time:WPMY-1 cells at 48 and 72h, WPE1-NA22 cells at 72 hours, BPH-1 cells at 48 and 72h, LNCaP cells at 48 and 72h
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Result:Reduced cell viability in all prostate cell lines, with the exception of the PC-3 cells.
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Cell Line:WPE1-NA22, BPH-1, LNCaP and VCaP
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Concentration:10 μM
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Incubation Time:24, 48 and 72 h
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Result:Induced a significant increase on caspase 3/7 activation.
In Vivo
Degarelix 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats, castrated[3]
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Dosage:0.3, 1, 3 and 10 μg/kg or 12.5, 50, and 200 μg/kg
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Administration:Subcutaneous injection, once
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Result:Produced a dose-dependent and reversible decrease in plasma LH levels with a minimal effective dose of 3 μg/kg.
For the 50 μg/kg and 200 μg/kg doses, t1/2 of absorption values were 4 min and 30 min, Tmax values were 1 h and 5 h, and apparent plasma disappearance t1/2 values were 12 h and 67 h, respectively.
Produced a dose-dependent decrease in plasma testosterone levels with a minimal effective dose of 1 μg/kg.
Chemical Information
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CAS No. 934246-14-7
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Formula C82H103ClN18O16.xC2H4O2.xH2O
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Synonyms
FE 200486 acetate hydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Degarelix acetate hydrate Related Classifications
HY-16168B Related Classifications
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