Biological ActivityApelin biased agonist; exhibits bias for the G protein pathway. Stimulates endothelial NOS phosphorylation and expression, promotes proliferation, and attenuates apoptosis of human pulmonary arterial endothelial cells in vitro. Shows positive inotropic and vasodilatory effects in vivo and improves cardiac structure and function in a model of pulmonary arterial hypertension.
(Modification: Disulfide bridge: 1-6)
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Design, characterization, and first-in-human study of the vascular actions of a novel biased apelin receptor agonist.
Brame et al.
A novel cyclic biased agonist of the apelin receptor, MM07, is disease modifying in the rat monocrotaline model of pulmonary arterial hypertension.
Yang et al.
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