ELA-21 (human) 是一种 apelin 受体激动剂,pKi 为 8.52。
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High affinity apelin receptor agonist. Binds apelin receptors in left ventricle from normal and pulmonary arterial hypertensive (PAH) hearts (pKi values are 9.31 and 9.46, respectively). Bioactive fragment of ELA-32 . Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.
Yang et al (2017) Elabela/Toddler is an endogenous agonist of the apelin APJ receptor in the adult cardiovascular system, and exogenous administration of the peptide compensates for the downregulation of its expression in pulmonary arterial hypertension. Circulation 135 1160 PMID:28137936 |Deng et al (2015) Apela regulates fluid homeostasis by binding to the APJ receptor to activate Gi signaling. J.Biol.Chem. 290 18261 PMID:25995451
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