Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Targets |
GnRHR
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ln Vitro |
Degarelix, among the LHRH antagonists Cetrorelix (HY-P0009), Abarelix (HY-13534), and Ganirelix (HY-P1628), exhibits the least amount of histamine release and the weakest histamine-releasing properties[1]. Except for PC-3 cells, degarelix (1 nM-10 μM, 0-72 h) decreases cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1, and VCaP cells)[2].
Degarelix (10 μM, 0-72 h) uses apoptosis to directly affect the growth of prostate cells[2]. |
ln Vivo |
Degarelix (0-10 μg/kg; s.c.; once) reduces plasma levels of testosterone and LH in castrated rats in a dose-dependent manner[3].
Degarelix is stable when incubated in microsomes and cryopreserved hepatocytes from animal liver tissue. In rats and dogs, the majority of the degarelix dosage is excreted in the urine and feces in equal proportions (40–50% in each matrix) within 48 hours, while in monkeys, the main excretion routes are the feces (50%) and the kidneys (22%)[4]. |
Animal Protocol |
Male Sprague-Dawley rats, castrated
0.3, 1, 3 and 10 μg/kg or 12.5, 50, and 200 μg/kg Subcutaneous injection, once |
References |
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Molecular Formula |
C₈₂H₁₀₃CLN₁₈O₁₆
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Molecular Weight |
1632.26
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Exact Mass |
1630.75
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Elemental Analysis |
C, 60.34; H, 6.36; Cl, 2.17; N, 15.45; O, 15.68
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CAS # |
214766-78-6
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Related CAS # |
Degarelix-d7; Degarelix acetate hydrate; 934246-14-7
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Appearance |
Solid powder
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SMILES |
C[C@H](C(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC2=CC=C(C=C2)NC(=O)N)NC(=O)[C@H](CC3=CC=C(C=C3)NC(=O)[C@@H]4CC(=O)NC(=O)N4)NC(=O)[C@H](CO)NC(=O)[C@@H](CC5=CN=CC=C5)NC(=O)[C@@H](CC6=CC=C(C=C6)Cl)NC(=O)[C@@H](CC7=CC8=CC=CC=C8C=C7)NC(=O)C
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InChi Key |
MEUCPCLKGZSHTA-XYAYPHGZSA-N
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InChi Code |
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
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Chemical 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
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Synonyms |
Degarelix Free Base; HSDB 7817; HSDB7817; HSDB-7817
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~10 mg/mL (~6.1 mM)
H2O: ~5 mg/mL (~3.1 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (0.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (0.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (0.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.6126 mL | 3.0632 mL | 6.1265 mL | |
5 mM | 0.1225 mL | 0.6126 mL | 1.2253 mL | |
10 mM | 0.0613 mL | 0.3063 mL | 0.6126 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03689699 | Active Recruiting |
Drug: Nivolumab Drug: Degarelix Drug: BMS-986253 |
Prostate Cancer Adenocarcinoma of the Prostate |
Mark Stein | October 11, 2018 | Phase 1 Phase 2 |
NCT03069937 | Active Recruiting |
Drug: Docetaxel Drug: Degarelix |
Metastatic Prostatic Adenocarcinoma |
Medical University of South Carolina |
March 1, 2017 | Phase 2 |
NCT04301414 | Active Recruiting |
Drug: Degarelix Drug: BMS-986218 and Degarelix |
Prostate Cancer | Columbia University | February 25, 2020 | Early Phase 1 |
NCT01994239 | Active Recruiting |
Drug: Degarelix Radiation: Pelvic Radiotherapy |
Adenocarcinoma of Prostate | UNICANCER | December 2012 | Phase 2 |
NCT01542021 | Active Recruiting |
Drug: degarelix injection Drug: androgen deprivation therapy |
Prostate Cancer Prostatic Adenocarcinoma |
Memorial Sloan Kettering Cancer Center |
February 2012 | Not Applicable |
MTT assay showing the viability of prostate cell lines following treatment with the GnRH antagonist, degarelix. PLoS One . 2015 Mar 26;10(3):e0120670. td> |
PLoS One . 2015 Mar 26;10(3):e0120670. td> |
Gene ontology classification (based on biological processes) of degarelix-deregulated genes on BPH-1 cells. PLoS One . 2015 Mar 26;10(3):e0120670. td> |