2. GPCR/G Protein Apoptosis
  3. GnRH Receptor Apoptosis
  4. Degarelix acetate hydrate

Degarelix acetate hydrate  (Synonyms: 地加瑞克醋酸水合物)

目录号: HY-16168B
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摩尔计算器

Degarelix acetate hydrate 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 acetate hydrate 可用于前列腺癌的研究。

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Degarelix acetate hydrate Chemical Structure

Degarelix acetate hydrate Chemical Structure

CAS No. : 934246-14-7

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Degarelix acetate hydrate 的其他形式现货产品:

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Other Forms of Degarelix acetate hydrate:

Degarelix acetate hydrate 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Degarelix acetate hydrate is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research[1].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Degarelix acetate hydrate 相关抗体:

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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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, t1/2 of absorption values were 4 min and 30 min, Tmax values were 1 h and 5 h, and apparent plasma disappearance t1/2 values 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.
Clinical Trial
Formula

C82H103ClN18O16.xC2H4O2.xH2O
CAS 号
中文名称

地加瑞克醋酸水合物
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Degarelix acetate hydrate 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Degarelix acetate934246-14-7地加瑞克醋酸水合物GnRH ReceptorApoptosisGonadotropin releasing hormone receptorGNRHRprostate cancerLHRHluteinizing hormone-releasing hormoneInhibitorinhibitorinhibit

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