Degarelix 是一种竞争性的、可逆的促性腺激素释放激素受体 (GnRHR/LHRHR) 拮抗剂。Degarelix 可用于前列腺癌的研究。
| 生物活性 | Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix can be used for prostatecancerresearch[1]. |
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体外研究
(In Vitro) | Degarelix shows only very weak histamine-releasing properties and the lowest capacity for histamine release among the antagonists of LHRH, including Cetrorelix (HY-P0009), Abarelix (HY-13534), and Ganirelix (HY-P1628)[1].
Degarelix (1 nM-10 μM, 0-72 h) reduces cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1, VCaP cells), with the exception of the PC-3 cells[2].
Degarelix (10 μM, 0-72 h) exerts a direct effect on prostate cell growth through apoptosis[2].
Cell Viability Assay[2] | Cell Line: | WPMY-1, WPE1-NA22, BPH-1, LNCaP and VCaP | | Concentration: | 1 nM-10 μM | | Incubation Time: | WPMY-1 cells at 48 and 72h, WPE1-NA22 cells at 72 hours, BPH-1 cells at 48 and 72h, LNCaP cells at 48 and 72h | | Result: | Reduced cell viability in all prostate cell lines, with the exception of the PC-3 cells. |
Apoptosis Analysis[2] | Cell Line: | WPE1-NA22, BPH-1, LNCaP and VCaP | | Concentration: | 10 μM | | Incubation Time: | 24, 48 and 72 h | | Result: | Induced a significant increase on caspase 3/7 activation. |
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体内研究
(In Vivo) | Degarelix (0-10 μg/kg; s.c.; once) decreases plasma LH levels and plasma testosterone levels in a dose-dependent manner in castrated rats[3].
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%)[4].
| Animal Model: | Male Sprague-Dawley rats, castrated[3] | | Dosage: | 0.3, 1, 3 and 10 μg/kg or 12.5, 50, and 200 μg/kg | | Administration: | Subcutaneous injection, once | | Result: | Produced a dose-dependent and reversible decrease in plasma LH levels with a minimal effective dose of 3 μg/kg.
For the 50 μg/kg and 200 μg/kg doses, t1/2of absorption values were 4 min and 30 min, Tmaxvalues were 1 h and 5 h, and apparent plasma disappearance t1/2values were 12 h and 67 h, respectively.
Produced a dose-dependent decrease in plasma testosterone levels with a minimal effective dose of 1 μg/kg. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Sealed storage, away from moisture | Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 10 mg/mL(6.13 mM;Need ultrasonic) H2O : 5 mg/mL(3.06 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 0.6126 mL | 3.0632 mL | 6.1265 mL | | 5 mM | 0.1225 mL | 0.6126 mL | 1.2253 mL | | 10 mM | --- | --- | --- |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1 mg/mL (0.61 mM); Clear solution
此方案可获得 ≥ 1 mg/mL (0.61 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 1 mg/mL (0.61 mM); Clear solution
此方案可获得 ≥ 1 mg/mL (0.61 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 1 mg/mL (0.61 mM); Clear solution
此方案可获得 ≥ 1 mg/mL (0.61 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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