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Degarelix

Degarelix (INN) or degarelix acetate (USAN) (trade name Firmagon) has an immediate onset of action, binding to gonadotropin-releasing hormone (GnRH) receptors in the pituitary gland and blocking their interaction with GnRH. This induces a fast and profound reduction in luteinising hormone (LH), follicle-stimulating hormone (FSH) and in turn, testosterone suppression. Testosterone is a male hormone that promotes growth of many prostate tumours..

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CAT No: 10-101-132

CAS No: 214766-78-6

Synonyms/Alias: Degarelix;214766-78-6;Firmagon;Uglypeptide1;SX0XJI3A11;FE200486;UNII-SX0XJI3A11;CHEMBL415606;FE-200486 (free base);HSDB 7817;FE200486 ANHYDROUS FREE BASE;FE200486 (AS ACETATE SALT);FE-200486 ANHYDROUS FREE BASE;DEGARELIX (MART.);DEGARELIX [MART.];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-;degarelixum;Degarelix [INN];Degarelix (Standard);Degarelix (acetate)?;DEGARELIX [MI];Degarelix (INN/USAN);DEGARELIX [HSDB];DEGARELIX [USAN];DEGARELIX [VANDF];DEGARELIX [WHO-DD];DEGARELIX [EMA EPAR];Degarelix [USAN:INN:BAN];GTPL5585;SCHEMBL1397034;DEGARELIX ACETATE [JAN];SCHEMBL21050504;L02BX02;CHEBI:135961;DTXSID801026401;GLXC-26186;HY-16168AR;BDBM50102450;HY-16168A;NSC771648;AKOS030526717;CS-5350;DB06699;NSC-771648;AS-82636;D08901;F85338;EN300-20626108;Q1182795;Ac-D-Nal-[D-(pCl)Phe]-D-Pal-Ser-[Aph(DHor)]-D-[Aph(Cbm)]-Leu-ILys-Pro-DAla-NH2;Ac-D-2Nal-D-Phe(4-Cl)-D-3Pal-Ser-Phe(4-S-dihydroorotamido)-D-Phe(4-ureido)-Leu-Lys(iPr)-Pro-D-Ala-NH2;Acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ILys-prolyl-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-N(sup 6)-(1-methylethyl)-L-lysyl-L-prolyl-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-D-alaninamide;

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Specification Technical Data Publications Customer reviews and Q&A
M.F/FormulaC82H103ClN18O16
M.W/Mr.1632.3
SequenceOne Letter Code:XXXSXXLXPA
Three Letter Code:Ac-D-2Nal-D-Phe(4-Cl)-D-3Pal-Ser-Phe(4-S-dihydroorotamido)-D-Phe(4-ureido)-Leu-Lys(iPr)-Pro-D-Ala-NH2
Long-term Storage ConditionsH2O : 25 mg/mL (15.32 mM; Need ultrasonic)
Shipping ConditionRoom temperature in continental US; may vary elsewhere.
InChIInChI=1S/C82H103ClN18O16/c1-45(2)35-60(72(107)92-59(16-9-10-33-87-46(3)4)80(115)101-34-12-17-68(101)79(114)88-47(5)70(84)105)93-74(109)63(38-51-23-30-58(31-24-51)91-81(85)116)95-76(111)64(39-50-21-28-57(29-22-50)90-71(106)66-42-69(104)100-82(117)99-66)97-78(113)67(44-102)98-77(112)65(41-53-13-11-32-86-43-53)96-75(110)62(37-49-19-26-56(83)27-20-49)94-73(108)61(89-48(6)103)40-52-18-25-54-14-7-8-15-55(54)36-52/h7-8,11,13-15,18-32,36,43,45-47,59-68,87,102H,9-10,12,16-17,33-35,37-42,44H2,1-6H3,(H2,84,105)(H,88,114)(H,89,103)(H,90,106)(H,92,107)(H,93,109)(H,94,108)(H,95,111)(H,96,110)(H,97,113)(H,98,112)(H3,85,91,116)(H2,99,100,104,117)/t47-,59+,60+,61-,62-,63-,64+,65-,66+,67+,68+/m1/s1
InChI KeyMEUCPCLKGZSHTA-XYAYPHGZSA-N

1. Oleic acid and glucose regulate glucagon-like peptide 1 receptor expression in a rat pancreatic ductal cell line

2. GLP-1, exendin-4 and C-peptide regulate pancreatic islet microcirculation, insulin secretion and glucose tolerance in rats

3. Spatiotemporal delivery of nanoformulated liraglutide for cardiac regeneration after myocardial infarction

4. Immune responses to peptides containing homocitrulline or citrulline in the DR4-transgenic mouse model of rheumatoid arthritis

5. Glucagonlike peptide 2 analogue teduglutide: stimulation of proliferation but reduction of differentiation in human Caco-2 intestinal epithelial cells

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