CB5064 Analogs act as agonists of the apelin receptor. CB5064 Analogs have been shown to:
Apelin is an endogenous peptide produced and secreted by several cell types, including fat (adipose tissue) and muscle cells, that activates the apelin receptor (APJ), a key cell surface receptor. Apelin/APJ axis is involved in protective regulation of fluid homeostasis, cardiovascular function, and metabolism. Activation of APJ, which is broadly expressed but particularly abundant in pulmonary and cardiac tissues, is known to be protective in animal models of ARDS, thrombosis, stroke and sepsis. In addition to its protective effects in lung injury, apelin has also been shown to reduce body weight and improve insulin sensitivity in obese mice.
Apelin itself is a poor drug candidate due to its relative instability and short half-life. Our CB5064 Analogs, while structurally distinct from apelin, have shown effects comparable, and in some cases superior, to those seen with apelin in mouse models of ARDS.