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Degarelix Acetate

D-Alaninamide,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-ly

CAS: 214766-78-6

Molecular Formula: C82H103ClN18O16

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Degarelix Acetate - Names and Identifiers

Name D-Alaninamide,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-ly
Synonyms FirMagon
Firmagon
Degarelix
DEGARELIX
Degarelix acetate
Degarelix acetate salt
Degarelix, Degarelix acetate
Degarelix acetate(FE-200486,Degarelix)
N-Acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-4-[2,6-dioxohexahydropyrimidin-4(S)-ylcarboxamido]-L-phenylalanyl-4-ureido-D-phenylalanyl-L-leucyl-N6-isopropyl-L-lysyl-L-prolyl-D-alaninamide acetate
D-Alaninamide,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-ly
D-Alaninamide, N-acetyl-3-(naphtalen-2-yl)-D-alanyl-4-chloro-D-phenylalanyl-3-(pyridin-3-yl)-D-alanyl-L-seryl-4-((((4S)-2,6-dioxohexahydropyrimidin-4-yl)carbonyl)amino)-L-phenylalanyl-4-(carbamoylamino)-D-phenylalanyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-
CAS 214766-78-6
EINECS 807-277-4

Degarelix Acetate - Physico-chemical Properties

Molecular FormulaC82H103ClN18O16
Molar Mass1632.26
Density1.325±0.06 g/cm3(Predicted)
pKa10.38±0.40(Predicted)
Storage ConditionKeep in dark place,Inert atmosphere,Store in freezer, under -20°C
In vitro study Degarelix acts directly on the pituitary receptors for luteinizing hormone-releasing hormone (LHRH), blocking the action of endogenous LHRH. The use of degarelix eliminates the initial undesirable surge in gonadotropin and testosterone levels, which is produced by agonists of LHRH. Degarelix treatment reduces cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1 cells, VCaP cells), with the exception of the PC-3 cells. The GnRH antagonist degarelix exerts a direct effect on prostate cell growth through apoptosis.
In vivo study At single subcutaneous injections of 0.3 to 10 μg/kg in rats, degarelix produces a dose-dependent suppression of the pituitary-gonadal axis as revealed by the decrease in plasma luteinizing hormone (LH) and testosterone levels. Duration of LH suppression increases with the dose: in the rat, significant suppression of LH lasted 1, 2, and 7 days after a single subcutaneous injection of degarelix at 12.5, 50, or 200 μg/kg, respectively. Degarelix 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%).

Degarelix Acetate - Preparation solution concentration reference

 1mg5mg10mg
1 mM0.613 ml3.063 ml6.126 ml
5 mM0.123 ml0.613 ml1.225 ml
10 mM0.061 ml0.306 ml0.613 ml
5 mM0.012 ml0.061 ml0.123 ml
Last Update：2024-01-02 23:10:35

Degarelix Acetate - Reference Information

Overview Diagarek acetate is a synthetic gonadotropin-releasing hormone (GnRH) receptor antagonist, which reversibly binds to the GnRH receptor of the pituitary gland to reduce the release of gonadotropins and testosterone, thereby exerting an anti-prostate cancer effect.
Antagonist of prostate cancer GnRH Degarek (trade name: Fermong®) is the latest generation of GnRH antagonist, which incorporates P-urylphenylalanine at the 5,6 positions of its molecule. The change of chemical structure prolongs the action time of the drug while avoiding the hypersensitivity caused by histamine release. reaction.
The clinical efficacy, safety and long-term medication of Dijarik have been verified by many clinical trials, and it is currently the most widely used GnRH antagonist. For advanced prostate cancer bone metastasis, Dijarek also shows good superiority. Studies have shown that patients with prostate cancer bone metastasis have significantly reduced plasma alkaline phosphatase (S-ALP) compared with GnRH agonist treatment after 1 year of treatment with Dijarek, and the S-ALP is often increased, which is often related to bone metastasis.
In November 2018, the National Medical Products Administration (NMPA) approved the listing of Garrick for androgen-dependent prostate cancer patients, which is undoubtedly a major benefit for prostate cancer patients in my country.
Mechanism of Action Degarek is a gonadotropin-releasing hormone (GnRH) receptor inhibitor drug developed by Denmark Huiling Pharmaceutical Co., Ltd., which reversibly inhibits the pituitary GnRH receptor to reduce the release of gonadotropins and then inhibit the release of testosterone. Digarek delays the growth and deterioration of prostate cancer by inhibiting testosterone, which is essential for the continued growth of prostate cancer. The initial stage of using hormones to treat prostate cancer to reduce testosterone concentration causes a surge in testosterone concentration. This initial stimulation of the hormone receptor can temporarily promote tumor growth instead of inhibiting it, while Digarek will not.
Use Degalac acetate is a gonadotropin-releasing hormone receptor blocker, which has been approved in the United States and Europe respectively For the treatment of advanced (hormone-dependent) prostate cancer, it is approved for the treatment of prostate cancer in Japan.
biological activity Degarelix is a competitive, reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
target GnRHR
toxic substance data information provided by: pubchem.ncbi.nlm.nih.gov (external link)
Last Update：2024-04-09 02:00:07
Degarelix Acetate
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Product Name: D-Alaninamide,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-ly Request for quotation
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Product Name: D-Alaninamide,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-ly Request for quotation
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Jiangsu Pules Biotechnology Co.,Ltd.
Product Name: D-Alaninamide,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-ly Request for quotation
CAS: 214766-78-6
Tel: 17505222756
Email: pules.cn@gmail.com
Mobile: +86-17551318830
Wechat: 17505222756
Hubei YoungXin Pharmaceutical Tech Co.,Ltd.
Spot supply
Product Name: Degarelix Visit Supplier Webpage Request for quotation
CAS: 214766-78-6
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
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Wechat: 15671228036
Hefei TNJ Chemical Industry Co.,Ltd.
Product Name: D-Alaninamide,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-ly Request for quotation
CAS: 214766-78-6
Tel: 0086-551-65418684
Email: sales@tnjchem.com
　　　　 info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840 Click to send a QQ message
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
Shanghai Yuanye Bio-Technology Co., Ltd.
Spot supply
Product Name: DEGARELIX Visit Supplier Webpage Request for quotation
CAS: 214766-78-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
Wechat: 18301782025
Shanghai Worldyang Chemical Co.,Ltd.
Product Name: D-Alaninamide,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-ly Request for quotation
CAS: 214766-78-6
Tel: +86-21-56795779
Email: charles7788@worldyachem.com
Mobile: +86-13651600618
QQ: 2850607228 Click to send a QQ message
Wechat: 13651600618
WhatsApp: +8613651600618
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Degarelix Acetate
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