Description
A GnRH receptor antagonist (IC50 = 0.1 nM); inhibits GnRH-induced arachidonic acid release in CHO cells expressing human recombinant or monkey recombinant GnRH (IC50s = 0.1 and 10 nM, respectively), but not the rat GnRH receptor; inhibits LH release in monkey pituitary cells stimulated ex vivo with GnRH (IC50 = 36 nM); sufugolix reduces increases in plasma LH following castration in male cynomolgus monkeys at 10 and 30 mg/kg; lowers serum LH, estradiol, and progesterone levels in female cynomolgus monkeys at 90 mg/kg
Formal name: N-[4-[1-[(2,6-difluorophenyl)methyl]-1,2,3,4-tetrahydro-5-[[methyl(phenylmethyl)amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-N’-methoxy-urea
Synonyms: TAK-013
Molecular weight: 667.7
CAS: 308831-61-0
Purity: ≥95%
Formulation: A solid
Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors||Research Area|Endocrinology & Metabolism|Reproductive Biology
