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Degarelix Acetate

名称
Degarelix Acetate
分子结构式
CAS号
214766-78-6
分子量
1632.26
分子式
C82H103ClN18O16
短序列号
Ac-D-2-Nal-D-4-Cl-F-D-3-Pal-S-4-Aph(Hor)-4-D-Aph(Cbm)-L-K(ipr)-Pa-NH2
序列号
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
国际标识符代码
MEUCPCLKGZSHTA-XYAYPHGZSA-N
纯度
95%
作用靶点
GnRH Receptor;Apoptosis
DMSO溶解度
10 mg/mL
水中溶解度
5 mg/m
引用文献
[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.
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Degarelix acetate is a reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist. Degarelix reduces the secretion of luteinizing hormone (LH) and testosterone via blocking GnRHR. Degarelix can be used for the treatment of prostate cancer.