生物活性：Relugolix-d6 is deuterium labeled Relugolix. 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)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].
体外研究(In Vitro)：Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Relugolix-d6 相关抗体:
Prolactin Receptor Antibody (YA2411)
Prolactin Antibody (YA1586)
GCDFP 15 Antibody (YA2242)
分子量：629.67
Formula：C29H21D6F2N7O5S
非标记 CAS：737789-87-6
性状：固体
中文名称：瑞卢戈利-d6
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：Powder：-20°C：3 years，4°C：2 years
In solvent：-80°C：6 months，-20°C：1 month
纯度 & 产品资料
Data Sheet (521 KB)
产品使用指南 (1538 KB)
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
 [Content Brief]
[2]. 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 Antagonist of the Human Gonadotropin-Releasing Hormone Receptor. doi/10.1021/jm200216q
[3]. 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. Eur J Pharmacol. 2014 Jan 15;723:167-74.
 [Content Brief]