| Identification | Back Directory | [Name]
Fe 200486 | [CAS]
934016-19-0 | [Synonyms]
Fe 200486
Reaxys ID: 26024935
Degarelix Acetate-d7
AUTFSFUMNFDPLH-KYMMNHPFSA-N
DEGARELIX (ACETATE);FE 200486
D-Alaninamide, N-acetyl-3-(naphtalen-2-yl)-D-alanyl-4-chloro-D-phenylalanyl-3-(pyridin-3-yl)-D-alanyl-L-seryl-4-((((4S)-2,6-dioxohexahydropyrimidin-4-yl)carbonyl)amino)-L-phenylalanyl-4-(carbamoylamino)-D-phenylalanyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-, acetate (1:1) | [Molecular Formula]
C84H107ClN18O18 | [MDL Number]
MFCD16879085 | [MOL File]
934016-19-0.mol | [Molecular Weight]
1692.34 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 0.25 mg/ml; PBS (pH 7.2): 10 mg/ml | [form ]
A crystalline solid | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
Degarelix acetate (FE 200486) is a decapeptide that shows high affinity/selectivity to human gonadotropin-releasing hormone (GnRH) receptor (IC50 = 3 nM). Degarelix acetate (FE 200486) is used for the research of prostate cancer[1][2]. | [Biological Activity]
Degarelix acetate (FE200486) is a gonadotropin-/luteinizing hormone-/follicle-stimulating hormone-releasing hormone (GnRHLHRHFSH-RH) receptor antagonist th at inhibits plasma testosterone for more than 40 days following a single s.c. dosage of 2 mg/kg in rats and monkeysshowing longer in vivo duration than abarelixganirelixcetrorelixazaline B or D-Trp6-LHRHand exhibiting only weak histamine-releasing potency in isolated r at mast cells. Bi-weekly s.c. dosing (2 mg/kg) is efficacious in suppressing the growth of human prostate cancer PAC120 xenograft-derived tumors in mice in vivo. | [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[5].
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%)[6]. | Animal Model: | Male Sprague-Dawley rats, castrated[5]. | | Dosage: | 0.3, 1, 3 and 10 μg/kg or 12.5, 50, and 200 μg/kg. | | Administration: | Subcutaneous injection, once. | | Result: | 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.
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| [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. DOI:10.2147/OTT.S32426
[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. DOI:10.1371/journal.pone.0120670
[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. DOI:10.1124/jpet.301.1.95
[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. DOI:10.1124/dmd.111.039883 |
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Apino Pharma Co., Ltd.
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