Abarelix(Synonyms: 阿巴瑞克; R3827; PPI 149)

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Abarelix (Synonyms: 阿巴瑞克; R3827; PPI 149) 纯度: 96.27%

Abarelix (R3827) 是有效的促性腺激素释放激素 (GnRH) 拮抗剂,用于研究前列腺癌。

Abarelix(Synonyms: 阿巴瑞克; R3827;  PPI 149)

Abarelix Chemical Structure

CAS No. : 183552-38-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3894 In-stock
5 mg ¥1500 In-stock
10 mg ¥2500 In-stock
25 mg ¥5500 In-stock
50 mg ¥9500 询价
100 mg   询价  
200 mg   询价  

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Abarelix 相关产品

相关化合物库:

  • FDA-Approved Drug Library Mini

生物活性

Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.

体外研究
(In Vitro)

Abarelix (30 and 300 µg/mL) causes significantly increased histamine release[1]. Abarelix is the first GnRH antagonist to be developed, and can produce rapid and sustained decreases in testosterone to castrate levels without the need for co-administration of an antiandrogen, and with a very low complication rate in the short term[2]. Abarelix demonstrates to promptly and substantially reduce follicle-stimulating hormone levels to lower than LHRH agonist. Abarelix does not cause a surge in serum testosterone that can precipitate a flare phenomenon or worsening of disease, particularly dangerous for patients with metastatic, symptomatic disease, and produces medical castration more quickly[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

1416.06

Formula

C72H95ClN14O14

CAS 号

183552-38-7

Sequence Shortening

Ac-{d-2-Nal}-{d-4-Cpa}-{d-3-Pal}-S-{NMyr}-{d-Asp}-L-K(ipr)-P-{d-Ala}-NH2

中文名称

阿巴瑞克

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 14.2 mg/mL (10.03 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7062 mL 3.5309 mL 7.0618 mL
5 mM 0.1412 mL 0.7062 mL 1.4124 mL
10 mM 0.0706 mL 0.3531 mL 0.7062 mL

*

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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Koechling W, et al. A novel GnRH antagonist, causes minimal histamine release compared with abarelix in an ex vivo model of human skin samples. Br J Clin Pharmacol. 2010 Oct;70(4):580-7.

    [2]. Kirby RS, et al. Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4.

    [3]. Debruyne F, et al. Abarelix for injectable suspension: first-in-class releasing hormone antagonist for prostate cancer. Future Oncol. 2006 Dec;2(6):677-96.

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