TAK-683 (TFA)

TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively[1]. TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer[1][2][3].

C66H84F3N17O15

1412.47

O=C(N)[C@H](CC1=CNC2=C1C=CC=C2)NC([C@H](CCCNC(NC)=N)NC([C@H](CC(C)C)NC(NNC([C@H](CC3=CC=CC=C3)NC([C@H]([C@H](O)C)NC([C@H](CC(N)=O)NC([C@@H](CC4=CNC5=C4C=CC=C5)NC([C@@H](CC6=CC=C(O)C=C6)NC(C)=O)=O)=O)=O)=O)=O)=O)=O)=O.O=C(O)C(F)(F)F

Kisspeptin Receptor

10 mM in DMSO

Room temperature