A synthetic GNRHR antagonist
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Degarelix (acetate)

Item No. 24069

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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-D-alaninamide, monoacetate
CAS Number
934016-19-0
Synonyms
  • FE 200486
Molecular Formula
C82H103ClN18O16 • C2H4O2
Formula Weight
1692.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 0.25 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
226, 246 nm
SMILES
O=C(N[C@H](CC1=CC=C(Cl)C=C1)C(N[C@H](CC2=CN=CC=C2)C(N[C@@H](CO)C(N[C@@H](CC3=CC=C(NC([C@@H]4CC(NC(N4)=O)=O)=O)C=C3)C(N[C@H](CC5=CC=C(NC(N)=O)C=C5)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCNC(C)C)C(N6[C@H](C(N[C@@H](C(N)=O)C)=O)CCC6)=O)=O)=O)=O)=O)=O)=O)[C@H](NC(C)=O)CC7=CC8=CC=CC=C8C=C7.OC(C)=O
InChi Code
InChI=1S/C82H103ClN18O16.C2H4O2/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;1-2(3)4/h7-8,11,13-15,18-32,36,43,45-47,59-68,87,102H,9-10,12,16-17,33-35,37-42,44
InChi Key
AUTFSFUMNFDPLH-KYMMNHPFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

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    Product Description

    Degarelix is a synthetic gonadotropin-releasing hormone receptor (GNRHR) antagonist (IC50 = 3 nM in HEK293 cells expressing the human receptor).1 It inhibits the growth of WPMY-1, WPE1-NA22, BPH-1, and LNCaP prostate cell lines following a 72-hour incubation at a concentration of 10 μM via caspase activation and induction of apoptosis.2 In vivo, degarelix (2 mg/kg) decreases plasma testosterone levels in rats to castrate levels for the first 49 days post administration.1 It decreases tumor volume of Dunning R3327H prostate tumor flank implants in rats when administered at a dose of 1 mg/kg per month.3 Formulations containing degarelix have been used in the treatment of advanced prostate cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jiang, G., Stalewski, J., Galyean, R., et al. GnRH antagonists: A new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6. J. Med. Chem. 44(3), 453-467 (2001).

    2. Sakai, M., Martinez-Arguelles, D.B., Patterson, N.H., et al. In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonist degarelix on human prostate cell growth. PLoS One 10(3), e0120670 (2015).

    3. Princivalle, M., Broqua, P., White, R., et al. Rapid suppression of plasma testosterone levels and tumor growth in the dunning rat model treated with degarelix, a new gonadotropin-releasing hormone antagonist. J. Pharmacol. Exp. Ther. 320(3), 1113-1118 (2007).