Degarelix? , ≥99% , 214766-78-6

Synonym(s):
Ac-D2Nal-D4Cpa-D3Pal-Ser-4Aph(L-hydroorotyl)-D4Aph(carbamoyl)-Leu-ILys-Pro-DAla-NH2 acetate salt;ASP3550 acetate;FE 200486;FE200486

CAS NO.：214766-78-6

Empirical Formula: C82H103ClN18O16

Molecular Weight: 1632.26

MDL number: MFCD05860888

EINECS: 807-277-4

PRODUCT Properties

• Density: 1.325±0.06 g/cm3(Predicted)
• storage temp.: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
• solubility: DMSO:10.0(Max Conc. mg/mL);6.13(Max Conc. mM); H2O:25.0(Max Conc. mg/mL);15.32(Max Conc. mM)
• pka: 10.38±0.40(Predicted)
• form: Solid
• color: White to off-white
• Sequence: Ac-D-2-Nal-D-4-Cl-Phe-D-3-Pal-Ser-4-Aph(Hor)-4-D-Aph(Cbm)-Leu-Lys(ipr)-Pro-D-Ala-NH2
• InChIKey: MEUCPCLKGZSHTA-XYAYPHGZSA-N

Description and Uses

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.

Advanced hormone-dependent prostate carcinoma

Safety

• Symbol(GHS): GHS08
• Signal word: Danger
• Hazard statements: H360