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DEGARELIX is , while it's Molecular Formula is C82H103ClN18O16. Advanced hormone-dependent prostate carcinoma
The CAS number of DEGARELIX is 214766-78-6.
More information of DEGARELIX 214766-78-6 are:
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Synonyms |
Acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ILys-prolyl-alaninamide;Degarelix;Firmagon;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-lysyl-L-prolyl-; |
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CAS Number |
214766-78-6 |
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Molecular Formula |
C82H103ClN18O16 |
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Molecular Weight |
1632.28 |
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Density |
1.325 g/cm3 |
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PSA |
512.87000 |
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LogP |
7.56580 |
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Pka |
10.38±0.40(Predicted) |
Antagonists of GnRH have proven to be an effective therapy for hormonally regulated cancers, such as prostate and some types of breast. As analogs of GnRH, they bind competitively and reversibly to GnRH receptors in the pituitary gland, thereby blocking the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). In men, the reduction of LH triggers the ablation of testosterone secretion from the testes, and these castration-like levels have been essential in the effective management of advanced prostate cancer. In comparison to GnRH agonists, antagonists do not suffer from a potential flare of the disease as a result of an initial stimulation of the hypothalamic-pituitary-gonadal axis prior to down-regulation of the GnRH receptor. Moreover, GnRH antagonists provide beneficial effects more rapidly postdosing and result in a more efficient suppression of gonadotropin levels. With this in mind, degarelix acetate has been launched as a third-generation GnRH antagonist for the treatment of prostate cancer, and it joins other third-generation agents, ganirelix and cetronelix, on the market.
Articles related to DEGARELIX:
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Article |
Source |
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Overcoming Chemical Challenges in the Solid-Phase Synthesis of High-Purity GnRH Antagonist Degarelix. Part 2 |
Biondi, Barbara,Cabri, Walter,Formaggio, Fernando,Guryanov, Ivan,Orlandin, Andrea,Ricci, Antonio,Viola, Angelo , p. 274 - 278 (2020) |
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Overcoming Chemical Challenges in the Solid-Phase Synthesis of High-Purity GnRH Antagonist Degarelix. Part 1. |
Guryanov, Ivan,Orlandin, Andrea,Viola, Angelo,Biondi, Barbara,Badocco, Denis,Formaggio, Fernando,Ricci, Antonio,Cabri, Walter , p. 2746 - 2753 (2019) |
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