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

Degarelix acetate  (Synonyms: FE 200486)

目录号: HY-16168
产品使用指南

摩尔计算器

Degarelix acetate (FE 200486) 是一种对人类促性腺激素释放激素 (GnRH) 受体具有高亲和力/选择性的十肽(IC50 = 3 nM)。Degarelix acetate (FE 200486) 用于前列腺癌的研究。

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Degarelix acetate Chemical Structure

Degarelix acetate Chemical Structure

CAS No. : 934016-19-0

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Degarelix acetate 的其他形式现货产品:

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Degarelix acetate 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Degarelix acetate (FE 200486) is a decapeptide that shows high affinity/selectivity to human gonadotropin-releasing hormone (GnRH) receptor (IC50 = 3 nM). Degarelix acetate (FE 200486) is used for the research of prostate cancer[1][2].

体外研究
(In Vitro)

Degarelix (FE 200486) 有非常弱的组胺释放特性，并且在所有 LHRH 拮抗剂中，包括 Cetrorelix (HY-P0009)、Abarelix (HY-13534) 和 Ganirelix (HY-P1628)，其组胺释放能力最低[1]。
Degarelix (1 nM-10 μM, 0-72 小时) 会降低所有前列腺细胞系 (WPE1-NA22, WPMY-1, BPH-1, VCaP 细胞) 的细胞活力，PC-3 细胞除外[4]。
Degarelix (10 μM, 0-72 小时) 通过诱导凋亡直接影响前列腺细胞生长[4]。

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

Degarelix acetate 相关抗体:

Cell Viability Assay[4]

Cell Line: WPMY-1, WPE1-NA22, BPH-1, LNCaP and VCaP.
Concentration: 1 nM-10 μM.
Incubation Time: 48-72 h
Result: 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. Reduced cell viability in all prostate cell lines, with the exception of the PC-3 cells.

Apoptosis Analysis[4]

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 (FE 200486 free base) (0-10 μg/kg; 皮下注射; 一次) 以剂量依赖性方式降低去势大鼠的血浆 LH 水平和血浆睾酮水平[5]。
Degarelix (FE 200486 free base) 在动物肝脏组织的微粒体和冷冻保存的肝细胞中培养时是稳定的。在大鼠和狗中，大部分 Degarelix 剂量在 48 小时内通过尿液和粪便以相等的量（每种基质 40-50%）排泄，而在猴子中，主要的排泄途径是粪便 (50%) 和肾脏 (22%)[6]。

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

Animal Model: Male Sprague-Dawley rats, castrated[5].
Dosage: 0.3, 1, 3 and 10 μg/kg or 12.5, 50, and 200 μg/kg.
Administration: Subcutaneous injection, once.
Result: 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.
分子量

1692.31

Formula

C84H107ClN18O18
CAS 号
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 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Degarelix934016-19-0FE 200486FE200486FE-200486GnRH ReceptorGonadotropin releasing hormone receptorGNRHRgonadotropin-releasing hormoneGnRHprostate cancerInhibitorinhibitorinhibit

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