Relugolix Biological Activity
Description:Relugolix is a novel, non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist with IC50 of 0.33 nM in the presence of 40% fetal bovine serum, TAK-385 possesses higher affinity and potent antagonistic activity compared with TAK-013.target: GnRH [1]IC50: 0.33 nM [1]In vivo: In female knock-in mice, twice-daily oral administration of TAK-385 (100mg/kg) induces constant diestrous phases within the first week, decreases the uterus weight to ovariectomized levels and downregulated GnRH receptor mRNA in the pituitary after 4 weeks.
Molecular Formula:C29H27F2N7O5S
Molecular Weight:623.63
PSA:169.36000
LogP:3.96660