货号	规格	价格	上海	北京	珠海	重庆	武汉
S86365-1mg买3赠1	99.40%	￥180.00 S86365-1mg ￥180.00 现货（买3赠1）	3709 >10	-	-	-	-
S86365-5mg买3赠1	99.40%	￥280.00 S86365-5mg ￥280.00 现货（买3赠1）	746 >10	-	-	-	-
S86365-10mg买3赠1	99.40%	￥320.00 S86365-10mg ￥320.00 现货（买3赠1）	377 >10	-	-	-	-
S86365-25mg买3赠1	99.40%	￥375.00 S86365-25mg ￥375.00 现货（买3赠1）	154 >10	-	-	-	-
S86365-100mg买3赠1	≥98%	￥845.00 S86365-100mg ￥845.00 现货（买3赠1）	37 >10	-	-	-	-

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产品描述：

Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209). Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al

靶点：

IC50: 0.33 nM (human GnRH) IC50: 0.32 nM (monkey GnRH);GNRHReceptor

体内研究：

Relugolix (oral administration; 1-3 mg/kg; single dose for pharmacokinetic study) exhibits a good pharmacokinetic profile and obvious suppressive effects of circulating LH levels in monkeys at a dose of 1 mg/kg. The pharmacokinetic profile exhibits with 16.0 ng/mL, 2.7 h, and 90.1 ng for Cmax, Tmax, and AUCo, respectively in male cynomolgus monkeys Relugolix (oral administration; 3, 10 or 30 mg/kg; twice daily; 4 weeks) significantly decreases the testis weight, and reduces the ventral prostate weight at 3 mg/kg and decreases it to castrate levels at 10 mg/kg in male hGNRHR-knock-in mice. Relugolix (oral administration; 30, 100 or 200 mg/kg; twice daily; 4 weeks) induces constant diestrous phases in all mice within the first week at 100 mg/kg, and significantly decreases the weights of ovaries and uteri at this dose after 4 weeks in female hGNRHR-knock-in mice

参考文献：

1. Kazuhiro Miwa, et al. Discovery of 1-{4-[1-(2,6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonis 2. Daisuke Nakata, 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. E

溶解性：

Soluble in DMSO

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.604 ml	8.018 ml	16.035 ml
5 mM	0.321 ml	1.604 ml	3.207 ml
10 mM	0.16 ml	0.802 ml	1.604 ml
50 mM	0.032 ml	0.16 ml	0.321 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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