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瑞卢戈利 /Relugolix {[allProObj[0].p_purity_real_show]}

货号:A261708 同义名: TAK-385;RVT-601 Ambeed 开学季,买赠积分,赢豪礼

Relugolix is a non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist with IC50 of 0.33 nM in the presence of 40% fetal bovine serum. It possesses higher affinity and potent antagonistic activity compared with TAK-013.

Relugolix 化学结构 CAS号:737789-87-6
Relugolix 化学结构
CAS号:737789-87-6
Relugolix 3D分子结构
CAS号:737789-87-6
Relugolix 化学结构 CAS号:737789-87-6
Relugolix 3D分子结构 CAS号:737789-87-6
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Relugolix 纯度/质量文件 产品仅供科研

货号:A261708 标准纯度: {[allProObj[0].p_purity_real_show]}
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Relugolix 生物活性

描述 Gonadotropin-releasing hormone (GnRH) is a decapeptide, which is synthesized in the hypothalamus and plays a pivotal role in the secretion of gonadotropins, such as luteinizing hormone and follicle-stimulating hormone. Relugolix is a novel, non-peptide, orally active GnRH antagonist with IC50s of 0.33 and 0.32 nM for human and monkey GnRH receptor, respectively. In vivo, twice-daily oral administration of relugolix (10 mg/kg) for 4 weeks reduced the prostate weight to castrate levels in male knock-in mice. In female knock-in mice, twice-daily oral administration of relugolix (100 mg/kg) induced constant diestrous phases within the first week, decreased the uterus weight to ovariectomized levels and downregulated GnRH receptor mRNA in the pituitary after 4 weeks. Moreover, gonadal function of relugolix-treated knock-in mice began to recover after 5 days and almost completely recovered within 14 days after drug withdrawal in both sexes suggesting suppression the hypothalamic-pituitary-gonadal axis caused by relugolix is reversible[3].

Relugolix 参考文献

[1]MacLean DB, Shi H, et al. Medical Castration Using the Investigational Oral GnRH Antagonist TAK-385 (Relugolix): Phase 1 Study in Healthy Males. J Clin Endocrinol Metab. 2015 Dec;100(12):4579-87.

[2]Nakata D, Masaki T, et al. Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active, small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH receptor knock-in mice. Eur J Pharmacol. 2014 Jan 15;723:167-74.

[3]Nakata D, Masaki T, Tanaka A, Yoshimatsu M, Akinaga Y, Asada M, Sasada R, Takeyama M, Miwa K, Watanabe T, Kusaka M. Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active, small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH receptor knock-in mice. Eur J Pharmacol. 2014 Jan 15;723:167-74

Relugolix 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.60mL

0.32mL

0.16mL

8.02mL

1.60mL

0.80mL

16.04mL

3.21mL

1.60mL

Relugolix 技术信息

CAS号737789-87-6
分子式C29H27F2N7O5S
分子量 623.63
别名 TAK-385;RVT-601
运输蓝冰
存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(168.37 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

动物实验配方
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