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..
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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M.F/Formula | C82H103ClN18O16 |
M.W/Mr. | 1632.3 |
Sequence | One 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 Conditions | H2O : 25 mg/mL (15.32 mM; Need ultrasonic) |
Shipping Condition | Room temperature in continental US; may vary elsewhere. |
InChI | InChI=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 Key | MEUCPCLKGZSHTA-XYAYPHGZSA-N |
3. Implications of ligand-receptor binding kinetics on GLP-1R signalling
5. Autoinhibition and phosphorylation-induced activation of phospholipase C-γ isozymes
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