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Relugolix

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Chemical Structure| 737789-87-6 同义名 : TAK-385;RVT-601
CAS号 : 737789-87-6
货号 : A261708
分子式 : C29H27F2N7O5S
纯度 : 99%+
分子量 : 623.63
MDL号 : MFCD25976856
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：
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].
实验方案
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
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