| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Among LHRH antagonists, such as Cetrorelix, Abarelix, and Ganirelix, Degarelix has the lowest histamine-releasing capacity and only very weak histamine-releasing properties [1]. Regarding PC-3 cells, degarelix (1 nM–10 μM) decreases cell viability in all prostate cell lines (WPE1–NA22, WPMY-1, BPH-1, and VCaP cells) [2]. Through apoptosis, degarelix (10 μM, 0-72 hours) directly affects the growth of prostate cells [2].
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| ln Vivo |
In castrated rats, degarelix (0-10 μg/kg; subcutaneous injection; once) decreases plasma levels of LH and testosterone in a dose-dependent manner [3]. When incubated in cryopreserved hepatocytes derived from animal liver tissue, degarelix remains stable. The majority of the degarelix dose is excreted in rats and dogs within 48 hours via urine and feces in equal proportions (40–50% in each matrix); in contrast, in monkeys, the primary excretion routes are feces (50%) and kidney (22%)[4].
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| Cell Assay |
Cell viability assay[2]
Cell Types: WPMY-1, WPE1-NA22, BPH-1, LNCaP and VCaP Tested Concentrations: 1 nM-10 μM Incubation Duration: 48 hrs (hours) and 72 hrs (hours) for WPMY-1 cells, 72 hrs (hours) for WPE1-NA22 cells , BPH-1 cells (48 hrs (hours) and 72 hrs (hours)), LNCaP cells (48 hrs (hours) and 72 hrs (hours)) Experimental Results: Cell viability was diminished in all prostate cell lines except PC-3 cells. Apoptosis analysis[2] Cell Types: WPE1-NA22, BPH-1, LNCaP and VCaP Tested Concentrations: 10 μM Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Induced significant increase in caspase 3/7 activation. |
| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat, castrated [3]
Doses: 0.3, 1, 3 and 10 μg/kg or 12.5, 50 and 200 μg/kg Route of Administration: subcutaneous injection, once Experimental Results:Dose-dependent And the minimum reversible effective dose is 3 μg/kg to reduce plasma LH levels. For the 50 μg/kg and 200 μg/kg doses, absorption t1/2 values were 4 minutes and 30 minutes, Tmax values were 1 hour and 5 hrs (hrs (hours)), and apparent plasma disappearance t1/2 values were 12 hrs (hrs (hours)) and 67 hrs (hrs (hours)), respectively. The minimum effective dose is 1 μg/kg, and plasma testosterone levels decrease in a dose-dependent manner. |
| References |
[1]. Rick FG, et al. An update on the use of degarelix in the treatment of advanced hormone-dependent prostate cancer. Onco Targets Ther. 2013 Apr 16;6:391-402.
[2]. Sakai M, et al. In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonistdegarelix on human prostate cell growth. PLoS One. 2015 Mar 26;10(3):e0120670. [3]. Broqua P, et al. Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormoneantagonist: degarelix. J Pharmacol Exp Ther. 2002 Apr;301(1):95-102. [4]. Sonesson A, et al. Metabolite profiles of degarelix, a new gonadotropin-releasing hormone receptor antagonist, in rat, dog, and monkey. Drug Metab Dispos. 2011 Oct;39(10):1895-903. |
| Molecular Formula |
C₈₂H₁₀₃CLN₁₈O₁₆
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|---|---|
| Molecular Weight |
1632.26
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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 |
Typically exists as solids (or liquids in special cases) at room temperature
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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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| 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 (~6.13 mM)
H2O : ~5 mg/mL (~3.06 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.
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