MM 07

MM 07 is a biased apelin receptor agonist, with a K_D of 300 nM in CHO-K1 cells and a K_D of 172 nM in human heart. IC50 & Target:KD: 300 nM (apelin receptor in CHO-K1 cells), 172 nM (apelin receptor in human heart)^[1]. In Vitro: MM 07 competes with nanomolar affinities for binding of [Glp⁶⁵,Nle⁷⁵,Tyr⁷⁷] [¹²⁵I]apelin-13 to human apelin receptors in CHO-K1 cells (K_D, 300 nM) and human heart (K_D, 172 nM, n=3)^[1]. In Vivo: MM 07 causes a dose-dependent increase in cardiac output, and although there is a decrease in vascular resistance, this is without corresponding effects on BP. Administration of SNAP produces a profound fall in BP in both [Pyr¹]apelin-13 and MM 07-treated groups; however, although cardiac output is significantly increased in response to SNAP in the MM 07 group, it is significantly reduced in the [Pyr¹]apelin-13 group. Neither peptide causes a significant change in heart rate, respiratory rate, or temperature. Both [Pyr¹]apelin 13 and MM 07 increases peak velocity above basal levels^[1].