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Degarelix

Degarelix  Structure
CAS No.
214766-78-6
Chemical Name:
Degarelix
Synonyms
Degarelix acetate;FirMagon;Dikarek;DEGARELIX;Degarelix-d7;Peptides Acetate;Degarelix impurity;DEGARELIX USP/EP/BP;Degarelix acetate salt;Degarelix, Degarelix acetate
CBNumber:
CB52448443
Molecular Formula:
C82H103ClN18O16
Molecular Weight:
1632.26
MOL File:
214766-78-6.mol
MSDS File:
SDS
Modify Date:
2026/8/4 11:17:55

Degarelix Properties

Density 1.325±0.06 g/cm3(Predicted)
storage temp. Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
solubility DMSO:10.0(Max Conc. mg/mL);6.13(Max Conc. mM)
H2O:25.0(Max Conc. mg/mL);15.32(Max Conc. mM)
pka 10.38±0.40(Predicted)
form Solid
color White to off-white
Sequence Ac-D-2-Nal-D-4-Cl-Phe-D-3-Pal-Ser-4-Aph(Hor)-4-D-Aph(Cbm)-Leu-Lys(ipr)-Pro-D-Ala-NH2
InChIKey MEUCPCLKGZSHTA-XYAYPHGZSA-N

SAFETY

Risk and Safety Statements

Symbol(GHS)  Health Hazard (GHS08)
GHS08
Signal word  Danger
Hazard statements  H360
Hazardous Substances Data 214766-78-6(Hazardous Substances Data)

Degarelix price

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Degarelix Chemical Properties,Uses,Production

Description

Antagonists of GnRH have proven to be an effective therapy for hormonally regulated cancers, such as prostate and some types of breast. As analogs of GnRH, they bind competitively and reversibly to GnRH receptors in the pituitary gland, thereby blocking the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). In men, the reduction of LH triggers the ablation of testosterone secretion from the testes, and these castration-like levels have been essential in the effective management of advanced prostate cancer. In comparison to GnRH agonists, antagonists do not suffer from a potential flare of the disease as a result of an initial stimulation of the hypothalamic-pituitary-gonadal axis prior to down-regulation of the GnRH receptor. Moreover, GnRH antagonists provide beneficial effects more rapidly postdosing and result in a more efficient suppression of gonadotropin levels. With this in mind, degarelix acetate has been launched as a third-generation GnRH antagonist for the treatment of prostate cancer, and it joins other third-generation agents, ganirelix and cetronelix, on the market.

Uses

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

Clinical Use

Ferring launched degarelix acetate, a gonadotrophin-releasing hormone (GnRH) antagonist, in 2009 in the U.S. for the treatment of prostate cancer. The compound has been approved by the E.U. for the same indication, and in the same year it was launched in the UK and Germany. Degarelix has been developed as a one-month or three-month sustained-release injectable formulation. Compared to other GnRH antagonists, degarelix displays improved aqueous solubility, longer acting effects and weaker histamine-releasing properties.

Side effects

The most common adverse events included injection site reactions (pain, erythema, swelling, or induration), hot flashes, increased weight, and increases in serum levels of transaminases and gamma-glutamyltransferase. In addition to being contraindicated in patients with a previous hypersensitivity to degarelix, it should not be administered to women who are or may become pregnant as fetal harm can occur. Since long-term androgen deprivation therapy prolongs the QT interval, physicians should consider whether the benefits of degarelix outweigh the potential risks in patients with congenital long QT syndrome, electrolyte abnormalities, or congestive heart failure or in patients taking antiarrhythmic medications.

Degarelix Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 295)Suppliers
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Jigs Chemical ltd +919099003427 Gujarat, India 234 58 Inquiry
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Sichuan Hantongkuntai Biotechnology Co., LTD. 18981903347 China 235 58 Inquiry
Lotusland Life Sciences +8615821988213 China 2411 58 Inquiry
DEGARELIX N-Acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-4-[2,6-dioxohexahydropyrimidin-4(S)-ylcarboxamido]-L-phenylalanyl-4-ureido-D-phenylalanyl-L-leucyl-N6-isopropyl-L-lysyl-L-prolyl-D-alaninamide acetate 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- Degarelix acetate(FE-200486,Degarelix) Degarelix, Degarelix acetate Degarelix acetate salt D-Alaninamide,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-ly D-Alaninamide, 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- Degarelix impurity DEGARELIX USP/EP/BP Degarelix-d7 Dikarek Peptides Acetate D7-Degarelix Trifluoroacetate FirMagon Degarelix acetate 214766-78-6 217466-78-6 C82H103ClN18O16C2H4O2 C82H103N18O16Cl C82H103ClN18O16 API