Relugolix
CAS#: 737789-87-6
Description: Relugolix, also known as TAK-385, is a luteinizing hormone-releasing hormone (LH-RH) receptor antagonist administered orally. By preventing LH-RH from binding with the LH-RH receptor in the anterior pituitary gland and suppressing the secretion of luteinizing hormone (LH) and follicle stimulation hormone (FSH) from the anterior pituitary gland, TAK-385 controls the effect of LH and FSH on the ovary, reduces the level of estrogen in blood, which is known to be associated with the development of endometriosis and uterine fibroids, and is expected to improve the symptoms of these disorders.
Synonym: TAK385; TAK-385; TAK 385; Relugolix.
IUPAC/Chemical Name: 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
PRICE AND AVAILABILITY
THEORETICAL ANALYSIS
Name: Relugolix
CAS#: 737789-87-6
Chemical Formula: C29H27F2N7O5S
Exact Mass: 623.17624
Molecular Weight: 623.63
Elemental Analysis: C, 55.85; H, 4.36; F, 6.09; N, 15.72; O, 12.83; S, 5.14
TECHNICAL DATA
REFERENCES
1: Miwa K, Hitaka T, Imada T, Sasaki S, Yoshimatsu M, Kusaka M, Tanaka A, Nakata D, Furuya S, Endo S, Hamamura K, Kitazaki T. 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. J Med Chem. 2011 Jul 28;54(14):4998-5012. Epub 2011 Jun 23. PubMed PMID: 21657270.
