metastin

Potent endogenous ligand of the kisspeptin receptor (KISS1, GPR54). Binds with high affinity to rat and human KISS1 receptors with Ki values of 1.80 and 1.45 nM respectively. Inhibits chemotaxis, invasion and metastasis of human melanomas and breast carci

TAK-683 TFA, a potent full KISS1 receptor (KISS1R) agonist with a half-maximal inhibitory concentration (IC50) of 170 pM, exhibits enhanced metabolic stability. As a nonapeptide metastin analog, it demonstrates agonistic activities towards KISS1R, with effective concentration (EC50) values of 0.96 nM for humans and 1.6 nM for rats. In vivo, TAK-683 TFA reduces gonadotropin-releasing hormone (GnRH) levels in the hypothalamus and decreases plasma follicle-stimulating hormone (FSH), luteinizing hormone (LH), and testosterone levels. Given these effects, TAK-683 TFA holds promise for research into hormone-dependent prostate cancer.

KISS1-305, the Metastin/Kisspeptin analog, is a prototype peptide and a chemical probe. KISS1-305 has suboptimal KISS1R agonistic activity, and resists plasma protease degradation.KISS1-305 is a proto- type peptide that resists plasma protease degradation

TAK-683 acetate is a nonapeptide metastin analog and a potent full agonist of the KISS1 receptor (KISS1R), exhibiting IC 50 =170 pM and enhanced metabolic stability. This compound shows agonistic activities towards KISS1R, with EC 50 values of 0.96 nM and 1.6 nM for human and rat KISS1R, respectively. TAK-683 acetate effectively depletes GnRH in the hypothalamus and reduces plasma levels of FSH, LH, and testosterone in vivo, showcasing its potential for hormone-dependent prostate cancer research.

TAK-683 is an effective full KISS1 receptor agonist (IC50=170 pM). TAK-683 is a nonapeptide metastin analog, shows agonistic activities to KISS1R (EC50: 0.96 nM and 1.6 nM for human and rat, respectively).

Kisspeptin-54(human) TFA, also known as Metastin(human) TFA, is the natural ligand for the kisspeptin receptor (KISS1, GPR54). It demonstrates high affinity for both rat and human GPR54 receptors with dissociation constants (K i) of 1.81 nM and 1.45 nM, respectively. This compound plays a crucial role in inhibiting tumor metastasis and promoting the secretion of gonadotropins, as evidenced by references [1] [2].