Relugolix (TAK-385) | GnRH receptor inhibitor | Probechem Biochemicals

Chemical Structure : TAK-385

CAS No.: 737789-87-6

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TAK-385 (Relugolix)

货号: PC-20087Not For Human Use, Lab Use Only.

TAK-385 (Relugolix, TAK385) is a potent, orally active, non-peptide antagonist of human gonadotropin-releasing hormone (GnRH) receptor, inhibits GnRH-stimulated AA release from CHO cells expressing human GnRH receptor with IC50 of 0.85 nM.

规格	价格	库存
10 mg	￥880	In stock
25 mg	￥1480	In stock
50 mg	￥2480	In stock
100 mg	￥4280	In stock
250 mg		Get quote

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生物&药学活性

TAK-385 (Relugolix, TAK385) is a potent, orally active, non-peptide antagonist of human gonadotropin-releasing hormone (GnRH) receptor, inhibits GnRH-stimulated AA release from CHO cells expressing human GnRH receptor with IC50 of 0.85 nM.
TAK-385 exhibited strong binding affinity (IC50=0.32 nM) for monkey receptor comparable to that for the human receptor while displaying a 30000-fold decrease for the rat receptor (IC50=9800 nM).
TAK-385 displayed no significant activity in 134 different enzyme and radioligand binding assays.
TAK-385 showed potent in vitro GnRH antagonistic activity in the presence of fetal bovine serum (FBS) without CYP inhibition.
Oral administration of TAK-385 demonstrated the suppressive effect of the plasma luteinizing hormone levels in castrated cynomolgus monkeys at a 3 mg/kg dose for more than 24 h.

物理化学性质&存储条件

分子量	623.64
分子式	C29H27F2N7O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Miwa K, et al. J Med Chem. 2011 Jul 28;54(14):4998-5012.

TAK-385 (Relugolix)

生物&药学活性

物理化学性质&存储条件

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TAK-385 (Relugolix)

生物&药学活性

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