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Chemical Structure : TAK-385
CAS No.: 737789-87-6
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $228 | In stock | |
| 100 mg | $528 | In stock | |
| 200 mg | $828 | In stock | |
| 1 g | Get quote | ||
| 5 g | Get quote |
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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.
| M.Wt | 623.64 | |
| Formula | C29H27F2N7O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Miwa K, et al. J Med Chem. 2011 Jul 28;54(14):4998-5012.
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