For research use only. Not for therapeutic Use.
Relugolix (Cat No.:I004740) is a novel oral gonadotropin-releasing hormone (GnRH) receptor antagonist. It works by competitively binding to and blocking the GnRH receptors in the pituitary gland, which leads to the inhibition of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release. This, in turn, suppresses the production of estrogen and testosterone. Relugolix has been primarily investigated for its use in the management of hormone-sensitive conditions such as advanced prostate cancer, endometriosis, and uterine fibroids. Its ability to rapidly and effectively suppress sex hormone levels has demonstrated favorable outcomes in clinical trials, offering a promising treatment option for these conditions.
| Catalog Number | I004740 |
| CAS Number | 737789-87-6 |
| Molecular Formula | C29H27F2N7O5S |
| Purity | 98% |
| Target | GnRH Receptor |
| Target Protein | P30968 |
| Solubility | 10 mM in DMSO |
| Appearance | Solid |
| Storage | Dry, dark and at 2 - 8 °C for six months or -20°C for two years. |
| IC50 | IC50: 0.33 nM (human GnRH)IC50: 0.32 nM (monkey GnRH) |
| IUPAC Name | 1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea |
| InChI | InChI=1S/C29H27F2N7O5S/c1-36(2)14-19-24-26(39)38(22-12-13-23(42-3)34-33-22)29(41)37(15-18-20(30)6-5-7-21(18)31)27(24)44-25(19)16-8-10-17(11-9-16)32-28(40)35-43-4/h5-13H,14-15H2,1-4H3,(H2,32,35,40) |
| InChIKey | AOMXMOCNKJTRQP-UHFFFAOYSA-N |
| SMILES | CN(C)CC1=C(SC2=C1C(=O)N(C(=O)N2CC3=C(C=CC=C3F)F)C4=NN=C(C=C4)OC)C5=CC=C(C=C5)NC(=O)NOC |
| Reference | 1:Medical Castration Using the Investigational Oral GnRH Antagonist TAK-385 (Relugolix): Phase 1 Study in Healthy Males. MacLean DB, Shi H, Faessel HM, Saad F.J Clin Endocrinol Metab. 2015 Dec;100(12):4579-87. doi: 10.1210/jc.2015-2770. Epub 2015 Oct 26. PMID: 26502357 Free PMC Article<br /> |
