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Degarelix

CAS No.: 214766-78-6

Chemical Name:: Degarelix

Synonyms: Degarelix acetate;FirMagon;Dikarek;DEGARELIX;Degarelix-d7;Degarelix impurity;DEGARELIX USP/EP/BP;Degarelix acetate salt;Degarelix, Degarelix acetate;Degarelix acetate(FE-200486,Degarelix)

CBNumber:: CB52448443

Molecular Formula:: C82H103ClN18O16

Molecular Weight:: 1632.26

MOL File:: 214766-78-6.mol

Modify Date:: 2024/7/2 8:55:11

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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)	GHS08
Signal word	Danger
Hazard statements	H360

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

Degarelix Suppliers

Global( 220)Suppliers

Supplier	Tel	Country	ProdList	Advantage	Inquiry
Jigs Chemical ltd	+919099003427	Gujarat, India	239	58	Inquiry
AKASH PHARMA EXPORTS	+91-9388123451 +91-9846039283	Kerela, India	470	58	Inquiry
AURO PEPTIDES LTD	+91 (40) 6672 1200	New Delhi, India	10	58	Inquiry
CLEARSYNTH LABS LTD.	+91-22-45045900	Hyderabad, India	6351	58	Inquiry
AFINE CHEMICALS LIMITED	+86-0571-85134551	China	15395	58	Inquiry
Apextide Co Ltd	+86-15300650552 +86-15300650552	China	71	58	Inquiry
Zibo Hangyu Biotechnology Development Co., Ltd	+86-0533-2185556 +8617865335152	China	11027	58	Inquiry
Henan Bao Enluo International TradeCo.，LTD	+86-17331933971 +86-17331933971	China	2503	58	Inquiry
Nantong Guangyuan Chemicl Co,Ltd	+undefined17712220823	China	616	58	Inquiry
Alpha Biopharmaceuticals Co., Ltd	+86-15542445688	China	888	58	Inquiry

Supplier	Advantage
Jigs Chemical ltd	58
AKASH PHARMA EXPORTS	58
AURO PEPTIDES LTD	58
CLEARSYNTH LABS LTD.	58
AFINE CHEMICALS LIMITED	58
Apextide Co Ltd	58
Zibo Hangyu Biotechnology Development Co., Ltd	58
Henan Bao Enluo International TradeCo.，LTD	58
Nantong Guangyuan Chemicl Co,Ltd	58
Alpha Biopharmaceuticals Co., Ltd	58

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Degarelix N-L-phenylalanyl-L-2-amino-1-phenylpropane N-[4-(3-OXO-PROPYL)-PHENYL]-ACETAMIDE

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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 Degarelix acetate FirMagon Dikarek 214766-78-6 217466-78-6 C82H103ClN18O16C2H4O2 C82H103N18O16Cl C82H103ClN18O16 API