| 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 |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京