Degarelix
Based on 11 publication(s) in Google Scholar
Degarelix acetate (FE 200486) is a decapeptide that shows high affinity/selectivity to human gonadotropin-releasing hormone (GnRH) receptor (IC50 = 3 nM). Degarelix acetate Degarelix acetate (FE 200486) is used for the research of prostate cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.96%
- CAS 番号: 214766-78-6
- 分子式: C82H103ClN18O16
- 分子量:1632.26
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Degarelix
More- Nat Cell Biol. 2026 Apr;28(4):707-724. [Abstract]
- Cancer Lett. 2023 Jul 1:565:216209. [Abstract]
- Arterioscler Thromb Vasc Biol. 2024 Mar;44(3):698-719. [Abstract]
- FASEB J. 2023 Feb;37(2):e22772. [Abstract]
- J Immunol. 2023 Feb 15;210(4):496-503. [Abstract]
- Microb Pathog. 2024 Dec:197:107046. [Abstract]
- Prostate. 2021 Sep;81(12):902-912. [Abstract]
- Res Sq. 2025 Apr 07.
- SSRN. 2024 May 22.
- bioRxiv. 2023 May 23:2023.05.23.540590. [Abstract]
- Research Square Preprint. 2020 Mar 27.
Customer Validation & Images
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ELISA
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In Vivo Efficacy Study
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Histological Imaging/Staining
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
生物活性
製品説明
IC50 & Target
GnRHR[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.58 nM
Compound: 1
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Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
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[PMID: 16759096] |
| HEK293 | IC50 |
1.64 nM
Compound: 2
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Antagonism of GnRH response in HEK293 cells expressing human GnRH receptor
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptor
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[PMID: 16033265] |
| HEK293 | IC50 |
8.8 nM
Compound: 32
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Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
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[PMID: 11462984] |
| Mast cell | EC50 |
>1000 μg/mL
Compound: 1
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Histamine release in mast cells by ELISA
Histamine release in mast cells by ELISA
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[PMID: 16759096] |
体外実験
Degarelix (FE 200486 free base) shows only very weak histamine-releasing properties and the lowest capacity for histamine release among the antagonists of LHRH, including Cetrorelix (HY-P0009), Abarelix (HY-13534), and Ganirelix (HY-P1628)[1].
Degarelix (1 nM-10 μM, 0-72 h) reduces cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1, VCaP cells), with the exception of the PC-3 cells[2].
Degarelix (10 μM, 0-72 h) exerts a direct effect on prostate cell growth through apoptosis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:WPMY-1, WPE1-NA22, BPH-1, LNCaP and VCaP
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Concentration:1 nM-10 μM
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Incubation Time:WPMY-1 cells at 48 and 72h, WPE1-NA22 cells at 72 hours, BPH-1 cells at 48 and 72h, LNCaP cells at 48 and 72h
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Result:Reduced cell viability in all prostate cell lines, with the exception of the PC-3 cells.
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Cell Line:WPE1-NA22, BPH-1, LNCaP and VCaP
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Concentration:10 μM
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Incubation Time:24, 48 and 72 h
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Result:Induced a significant increase on caspase 3/7 activation.
体内実験
Degarelix (FE 200486 free base) is stable when incubated in microsomes and cryopreserved hepatocytes from animal liver tissue. In rat and dog, most of the degarelix dose is eliminated within 48 h via urine and feces in equal amounts (40–50% in each matrix), whereas in monkey the major route of excretion is fecal (50%) and renal (22%)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats, castrated[3]
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Dosage:0.3, 1, 3 and 10 μg/kg or 12.5, 50, and 200 μg/kg
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Administration:Subcutaneous injection, once
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Result:Produced a dose-dependent and reversible decrease in plasma LH levels with a minimal effective dose of 3 μg/kg.
For the 50 μg/kg and 200 μg/kg doses, t1/2 of absorption values were 4 min and 30 min, Tmax values were 1 h and 5 h, and apparent plasma disappearance t1/2 values were 12 h and 67 h, respectively.
Produced a dose-dependent decrease in plasma testosterone levels with a minimal effective dose of 1 μg/kg.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 214766-78-6
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性状 Solid
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分子量 1632.26
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分子式 C82H103ClN18O16
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Color White to off-white
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別名
FE 200486 free base
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (11)
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Journal Impact Factor
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Most Recent
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Nat Cell Biol
An extracellular vesicle-mediated mitochondrial transfer network critical for testosterone synthesis. [Abstract]2026 Apr;28(4):707-724. PMID: 41760931 -
Cancer Lett
SOX2 expression in prostate cancer drives resistance to nuclear hormone receptor signaling inhibition through the WEE1/CDK1 signaling axis. [Abstract]2023 Jul 1:565:216209. PMID: 37169162 -
Arterioscler Thromb Vasc Biol
FSH Is Responsible for Androgen Deprivation Therapy-Associated Atherosclerosis in Mice by Exaggerating Endothelial Inflammation and Monocyte Adhesion. [Abstract]2024 Mar;44(3):698-719. PMID: 38205641
Degarelix purchased from MedChemExpress. Usage Cited in: Arterioscler Thromb Vasc Biol. 2024 Mar;44(3):698-719. [Abstract]
Serum levels of testosterone and follicle-stimulating hormone (FSH) in mice were assessed by ELISA. Degarelix (Deg) (50 mg/kg; s.c.; once a month) rapidly reduced FSH and testosterone levels in high-fat diet–fed male ApoE−/− mice.
Degarelix purchased from MedChemExpress. Usage Cited in: Arterioscler Thromb Vasc Biol. 2024 Mar;44(3):698-719. [Abstract]
The Degarelix (Deg) (50 mg/kg; s.c.; once a month) group showed similar or even smaller atherosclerotic lesions in the aortic root and aortic tree of high-fat diet–fed male ApoE−/− mice compared with the saline group.
Degarelix purchased from MedChemExpress. Usage Cited in: Arterioscler Thromb Vasc Biol. 2024 Mar;44(3):698-719. [Abstract]
SmαA (smooth muscle α-actin) and F4/80 immunostaining (red) on the plaques of aortic roots of mice. Degarelix (Deg) (50 mg/kg; s.c.; once a month) barely changed macrophage contents, smooth muscle cells and collagen contents.
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FASEB J
Circadian disruption impairs glucose homeostasis in male but not in female mice and is dependent on gonadal sex hormones. [Abstract]2023 Feb;37(2):e22772. PMID: 36645117
Degarelix purchased from MedChemExpress. Usage Cited in: FASEB J. 2023 Feb;37(2):e22772. [Abstract]
Degarelix (25 mg/kg; s.c.; at days 1 and 29) decreased seminal vesicle and ovary weight, suppressed gonadal sex hormone production, and reduced rhythm strength and total food intake in male and female C57BL/6J mice.
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J Immunol
2023 Feb 15;210(4):496-503. PMID: 36548468 -
Microb Pathog
2024 Dec:197:107046. PMID: 39433139
Degarelix purchased from MedChemExpress. Usage Cited in: Microb Pathog. 2024 Dec:197:107046. [Abstract]
Degarelix (10 mg/kg; p.o.; once daily for 14 d) supplementation led to a lower bacterial burden and less granuloma formation in zebrafish adults infected with M. marinum compared to those fish treated with mock, while degarelix therapeutic effects were similar to RFP effects.
Degarelix purchased from MedChemExpress. Usage Cited in: Microb Pathog. 2024 Dec:197:107046. [Abstract]
BMDMs pretreated with degarelix (1 μM), aminoguanidine hydrochloride (AGHS, 100 μM), BafA1 (100 nM), NAC (5 mM), Z-VAD (20 μM), or 3-MA (5 mM) were infected with H37Rv (MOI = 2). At different time points after infection, bacterial survival was calculated by dividing the CFU at 24 h by the CFU at 3 h.
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Prostate
Gonadotropin-releasing hormone antagonist associated with lower cardiovascular risk compared with gonadotropin-releasing hormone agonist in prostate cancer: A nationwide cohort and in vitro study. [Abstract]2021 Sep;81(12):902-912. PMID: 34196430 -
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bioRxiv
Suppression of tumor cell lactate-generating signaling pathways eradicates murine PTEN/p53-deficient aggressive-variant prostate cancer via macrophage phagocytosis. [Abstract]2023 May 23:2023.05.23.540590. PMID: 37292972 -
溶剤 & 溶解度
体外:
DMSO : 10 mg/mL (6.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 5 mg/mL (3.06 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 12.5 mg/mL (7.66 mM); Clear solution; Need ultrasonic
プロトコル
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
純度とドキュメンテーション
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データシート (283 KB)
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- Français - FR (396 KB)
- Deutsch - DE (396 KB)
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取扱説明書 (2659 KB)
参考文献
[2]. Degarelix.
[3]. 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. [Content Brief]
[4]. 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. [Content Brief]
[5]. 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. [Content Brief]
[6]. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 0.6126 mL | 3.0632 mL | 6.1265 mL | 15.3162 mL |
| DMSO | 5 mM | 0.1225 mL | 0.6126 mL | 1.2253 mL | 3.0632 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Degarelix 関連分類
HY-16168A 関連分類
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