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Degarelix

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Chemical Structure| 214766-78-6 同义名 : Degarelix游离 ;Degarelix acetate
CAS号 : 214766-78-6
货号 : A890488
分子式 : C82H103ClN18O16
纯度 : 98%
分子量 : 1632.259
MDL号 : MFCD05860888
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(5.51 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5 mg/mL(3.06 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
描述 Blockage of gonadrotropin-releasing hormone (GnRH) receptor (GnRHR) leads to a decrease in both luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release from the pituitary, and subsequently testosterone production from testes is suppressed. Degarelix is a GnRHR antagonist used in patients with prostate cancer (PCa) who need androgen deprivation therapy (ADT). In vitro, cell viability of different prostate cells was decreased after 24, 48, or 72h of treatment with 10 μM degarelix. Furthermore, degarelix treatment induced a significant increase on caspase 3/7 activation compared to control in normal, hyperplasia, and cancer cells indicating that cells were undergoing apoptosis using the caspase cascade[3]. In vivo, at single subcutaneous injections of 0.3 to 10 μg/kg in rats, degarelix produced a dose-dependent suppression of the pituitary-gonadal axis as revealed by the decrease in plasma LH and testosterone levels[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.61mL

0.12mL

0.06mL

3.06mL

0.61mL

0.31mL

6.13mL

1.23mL

0.61mL
参考文献

[1]Sakai M, Martinez-Arguelles DB, et al. In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonist degarelix on human prostate cell growth. PLoS One. 2015 Mar 26;10(3):e0120670.

[2]Rick FG, Block NL, 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.

[3]Sakai M, Martinez-Arguelles DB, et al. In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonist degarelix on human prostate cell growth. PLoS One. 2015 Mar 26;10(3):e0120670

[4]Broqua P, Riviere PJ, Conn PM, Rivier JE, Aubert ML, Junien JL. Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormone antagonist: degarelix. J Pharmacol Exp Ther. 2002 Apr;301(1):95-102