Kisspeptin-234 trifluoroacetate salt

Kisspeptin-234 is a 10-amino acid peptide antagonist with potent neutral antagonist activity at GPR-54 and competes directly at the Kisspeptin-10 binding site. Kisspeptin-234 is the first reported antagonist for the kisspeptin-1/GPR-54 signaling system.

Gonadotropin-releasing hormone (GnRH) modulates the hypothalamic-pituitary-gonadal axis, enabling the brain to control reproductive processes. Kisspeptin-1 is a peptide neurotransmitter released from afferent neurons onto GnRH neurons, where it binds to and activates to the orphan receptor GPR-54 to regulate release of GnRH. Regulation of kisspeptin/GPR-54 signaling presents an opportunity for reproductive therapeutics above the level of GnRH and gonadotropin secretion. Pharmacological and selective tools are needed to better understand kisspeptin-1/GPR-54 signaling. Analogs of kisspeptin-10, a 10-amino acid portion of kisspeptin-1, were designed to be full and neutral antagonists of GPR-54.