Kisspeptin-54(human)

Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) binds to rat and human GPR54 receptors with K_i values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) inhibits tumor metastasis and stimulates the secretion of gonadotropin (LH) and testosterone^{[1][2][3][4][5][6][7][8]}. IC50 & Target:Ki: 1.81 nM (Rat GPR54) and 1.45 nM (Human GPR54)^[2] In Vitro:Kisspeptin-54(human) (1-100 nM, 4-48 h) stimulates aldosterone synthesis in human adrenal cells (H295R cells and fetal adrenal neocortex cells)^[3].
Kisspeptin-54(human) (1-10 μM, 12 h) suppresses migration of human pancreatic cancer cells (PANC-1) ^[4].
Kisspeptin-54(human) (10-1000 nM, 14-16 h for migration, 24-48 h for invasion) inhibits migration and invasion of human renal cell carcinoma cells (Caki-1 and ACHN) with overexpression of metastireceptor^[5].
In Vivo:Kisspeptin-54(human) (0.3-100 nmol/kg, i.p., 30 min before trunk blood and anterior pituitaries are collected) dose-dependently shows activation of the anterior pituitary release of LH in post-pubertal male rats^[6].
Kisspeptin-54(human) (0.3-30 nmol/kg, i.p.) produces a dose-dependent effect on c-fos mRNA levels in the anterior pituitary in various ages (PND15, PND30, and PND45) male rats^[6].
Kisspeptin-54(human) (0.1-30 nmol/kg, i.p., single) increases serum testosterone in mice, with the same potency as for mouse kisspeptins^[7].
Kisspeptin-54(human) (6.7 nmol/rat, s.c.) induces the release of gonadotropin via activation of the hypothalamic GnRH neurons in prepubertal female rats^[8].