Relugolix (TAK-385) 是一种有效的，具有口服活性，非肽性促性腺激素释放激素(GnRH) 的拮抗剂。与 TAK-013 (HY-100209 ) 相比，Relugolix 对人 (IC₅₀=0.33 nM) 和猴子 (IC₅₀=0.32 nM) 的受体具有高亲和力和强拮抗活性。Relugolix 用于性激素依赖性疾病的研究，如子宫内膜异位症、子宫肌瘤、前列腺癌等。

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 IC 50 =0.33 nM) and monkey receptor (IC 50 =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.

Solid

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

Relugolix exhibits strong binding affinity (IC50=0.32 nM) for the monkey receptor comparable to that for the human receptor (IC50=0.33 nM) while displaying a 30000-fold decrease for the rat receptor (IC50=9800 nM). The antagonistic in vitro activity of TAK-385 with respect to the human receptor (IC90=18 nM) exceeded that for the monkey receptor (IC90=1700 nM) by 95-fold in the presence of 40% serum.
has not independently confirmed the accuracy of these methods. They are for reference only.

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 C max , T max , and AUC o , 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 fema

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 100 mg/mL (160.35 mM; Need ultrasonic)配制储备液