KD: 300 nM (apelin receptor in CHO-K1 cells), 172 nM (apelin receptor in human heart)[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].
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 (KD, 300 nM) and human heart (KD, 172 nM, n=3)[1].
Kinase Assay
Cell Assay
Animal Administration
Rats[1]Rats (230-260 g), anaesthetized with 2% isoflurane, are given a single intravenous bolus (600 nM) of apelin or MM 07 (both n=3)[1].
References
[1]. Brame AL, et al. Design, characterization, and first-in-human study of the vascular actions of a novel biased apelin receptor agonist. Hypertension. 2015 Apr;65(4):834-40.
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