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Degarelix

* Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients.

Degarelix acetate is a reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist. Degarelix reduces the secretion of luteinizing hormone (LH) and testosterone via blocking GnRHR. Degarelix can be used for the treatment of prostate cancer.

Category

Peptide Inhibitors

Catalog number

BAT-010776

CAS number

214766-78-6

Molecular Formula

C82H103ClN18O16

Molecular Weight

1632.286

Size	Price	Stock	Quantity
10 mg	$199	In stock

Specification
Reference Reading

IUPAC Name

(4S)-N-[4-[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-[[(2R)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2R)-1-amino-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxo-6-(propan-2-ylamino)hexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[4-(carbamoylamino)phenyl]-1-oxopropan-2-yl]amino]-3-oxopropyl]phenyl]-2,6-dioxo-1,3-diazinane-4-carboxamide

Synonyms

Degarelix; Firmagon; FE-200486; FE 200486; FE200486; ASP-3550; ASP 3550; ASP3550; 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

Related CAS

934246-14-7 (acetate hydrate)

Purity

>98%

Density

1.3±0.1 g/cm3

Sequence

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

Storage

Store at -20°C

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

Canonical SMILES

CC(C)CC(C(=O)NC(CCCCNC(C)C)C(=O)N1CCCC1C(=O)NC(C)C(=O)N)NC(=O)C(CC2=CC=C(C=C2)NC(=O)N)NC(=O)C(CC3=CC=C(C=C3)NC(=O)C4CC(=O)NC(=O)N4)NC(=O)C(CO)NC(=O)C(CC5=CN=CC=C5)NC(=O)C(CC6=CC=C(C=C6)Cl)NC(=O)C(CC7=CC8=CC=CC=C8C=C7)NC(=O)C

1.[Histrelin acetate--the first once yearly LHRH agonist].

Altarac S1. Lijec Vjesn. 2011 Sep-Oct;133(9-10):320-2.

Long-acting synthetic luteinising hormone-releasing hormone agonists have become the mainstay for androgen-deprivation therapy, because they avoid the physical and psychological discomfort associated with orchidectomy and lack the potential cardiotoxicity associated with estrogens such as diethylstilbestrol. Currently available luteinising hormone-releasing hormone agonist analogues include leuprolide, goserelin, triptorelin, degarelix and buserelin were administered as either intramuscular or subcutaneous depot injections on a 1, 2, 3 or 6 months basis. Histrelin acetate is the first long-acting luteinising hormone-releasing hormone agonist available as a once-yearly subcutaneous implant.

2.Cardiovascular safety of degarelix: results from a 12-month, comparative, randomized, open label, parallel group phase III trial in patients with prostate cancer.

Smith MR1, Klotz L, Persson BE, Olesen TK, Wilde AA. J Urol. 2010 Dec;184(6):2313-9. doi: 10.1016/j.juro.2010.08.012. Epub 2010 Oct 16.

PURPOSE: We assessed the cardiovascular safety profile of degarelix, a new gonadotropin-releasing hormone antagonist.

3.Degarelix acetate for the treatment of prostate cancer.

Klotz L1. Drugs Today (Barc). 2009 Oct;45(10):725-30. doi: 1396674/dot.2009.45.10.1417873.

Pharmacological methods of achieving androgen deprivation for the treatment of prostate cancer have evolved. New strategies are focusing on avoidance of the undesirable effects of testosterone surges or flares associated with the initial stages of gonadotropin-releasing hormone (GnRH) agonists and the significant histamine-mediated side effects that can be associated with GnRH antagonists. Degarelix acetate (Firmagon; Ferring Pharmaceuticals) is a third-generation GnRH antagonist that has been shown to produce a significantly more rapid medical castration (without testosterone surge) and prostate-specific antigen response compared with GnRH agonists. The safety profile is comparable to GnRH agonists and anaphylactic reactions have not been reported. Degarelix is currently available as a 1-month subcutaneous injection and has been approved for the treatment of advanced prostate cancer.