TAK-683 TFA is a potent fullKISS1 receptor (KISS1R)agonist (IC₅₀=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R withEC₅₀values of 0.96 nM and 1.6 nM for human and rat, respectively^[1]. TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasmaFSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostatecancer^[1][2][3].

IC50: 170 pM (metastin/GPR54)^[1]

TAK-683 (subcutaneous injection; 0.008, 0.08, 0.8, or 8 μmol/ml/kg; once daily; 7 days) induces an increase in plasma luteinizing hormone and testosterone levels; however, after day 7, plasma hormone levels and genital organ weights are reduced^[1].
TAK-683 (subcutaneous injection; 10, 30, or 100 pmol/h; once daily; 4 weeks) provides a promising for suppressing reproductive functions and hormone-related diseases such as prostate cancer^[1].
TAK-683 (subcutaneous injection; 2.1-21 nmol/kg/day; once daily; 12 weeks) has a longer-term evaluation in prostate cancer model, serum concentrations of PSA is reduced in rats, PSA concentrations are reduced to below the limit of detection (0.5 ng/ml)) in all rats by day 14^[1].

1412.47

C₆₆H₈₄F₃N₁₇O₁₅

N-Acetyl-YWNTF{aza}L{Met-R}W-NH2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.