Fe 200486

Product Name: Fe 200486
CAS No.: 934016-19-0
Chemical Name: Fe 200486
Synonyms: Fe 200486;Reaxys ID: 26024935;Degarelix Acetate-d7;Degarelix Acetate Impurity;Degarelix acetate - Bio-X ?;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);N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-4-[[[(4S)-hexahydro-2,6-dioxo-4-pyrimidinyl]carbonyl]amino]-L-phenylalanyl-4-[(aminocarbonyl)amino]-D-phenylalanyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-D-alaninamide,monoacetate
CBNumber: CB82492669
Molecular Formula: C84H107ClN18O18
Formula Weight: 1692.34
MOL File: 934016-19-0.mol

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Fe 200486 Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P308+P313IF exposed or concerned: Get medical advice/attention.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML2856
Product name: Degarelix acetate
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $91.96
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML2856
Product name: Degarelix acetate
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $372.4
Updated: 2025/07/31

Cayman Chemical

Product number: 24069
Product name: Degarelix (acetate)
Purity: ≥98%
Packaging: 5mg
Price: $75
Updated: 2024/03/01

Cayman Chemical

Product number: 24069
Product name: Degarelix (acetate)
Purity: ≥98%
Packaging: 10mg
Price: $142
Updated: 2024/03/01

Cayman Chemical

Product number: 24069
Product name: Degarelix (acetate)
Purity: ≥98%
Packaging: 25mg
Price: $336
Updated: 2024/03/01

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Fe 200486 Chemical Properties,Usage,Production

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 (GnRH, LHRH, FSH-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 monkeys, showing longer in vivo duration than abarelix, ganirelix, cetrorelix, azaline B or D-Trp6-LHRH, and 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, t_1/2 of absorption values were 4 min and 30 min, T_max values were 1 h and 5 h, and apparent plasma disappearance t_1/2 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.

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

Fe 200486 Preparation Products And Raw materials

Raw materials

Preparation Products

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Fe 200486 Suppliers

China 22 India 1 Japan 1 United States 6 Global 30

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934016-19-0, Fe 200486Related Search:

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)

Fe 200486

AUTFSFUMNFDPLH-KYMMNHPFSA-N

Reaxys ID: 26024935

Degarelix Acetate-d7

DEGARELIX (ACETATE);FE 200486

N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-4-[[[(4S)-hexahydro-2,6-dioxo-4-pyrimidinyl]carbonyl]amino]-L-phenylalanyl-4-[(aminocarbonyl)amino]-D-phenylalanyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-D-alaninamide,monoacetate

Degarelix Acetate Impurity

Degarelix acetate - Bio-X ?

934016-19-0

C2H4O2C82H103ClN18O16