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S84434

DEGARELIX

源叶(MedMol) 99%
  • 英文名:
  • DEGARELIX
  • 别名:
  • 地加瑞克;醋酸地加瑞克;DEGARELIX;Degarelix acetate;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-urei
  • CAS号:
  • 214766-78-6
  • 分子式:
  • C82H103ClN18O16
  • 分子量:
  • 1632.28
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S84434-5mg 99% ¥1200.00元 9 - - - EA 加入购物车
源叶(MedMol) S84434-10mg 99% ¥2240.00元 5 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix can be used for prostate cancer research
  • 靶点: GnRHR;GNRHReceptor
  • 体内研究:
    Degarelix (0-10 μg/kg; s.c.; once) decreases plasma LH levels and plasma testosterone levels in a dose-dependent manner in castrated rats. 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%)
  • 参考文献:
    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.
  • 溶解性: DMSO  :  10  mg/mL  (6.13  mM;  Need  ultrasonic)    H2O  :  5  mg/mL  (3.06  mM;  ultrasonic  and  warming  and  heat  to  60°C)
  • 保存条件: -20°C,避光
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 0.613 ml 3.063 ml 6.126 ml
    5 mM 0.123 ml 0.613 ml 1.225 ml
    10 mM 0.061 ml 0.306 ml 0.613 ml
    50 mM 0.012 ml 0.061 ml 0.123 ml
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