Apelin-17 (K17F) is a potent and selective endogenous agonist of apelin receptor (apelin-R). Apelin-17 has 16 times higher affinity for apelin-R than apelin-13 (pE13F) (Ki = 0.05 versus 0.8 nM).
potent and selective endogenous agonist of apelin receptor (apelin-R)
Apelin and arginine-vasopressin (AVP) are conversely regulated by osmotic stimuli. We therefore hypothesized that activating the apelin receptor (apelin-R) with LIT01-196, a metabolically stable apelin-17 analog, may be beneficial for treating the Syndrome of Inappropriate Antidiuresis, in which AVP hypersecretion
Apelin peptides mediate beneficial effects on the cardiovascular system and are being targeted as potential new drugs. However, apelin peptides have extremely short biological half-lives, and improved understanding of apelin peptide metabolism may lead to the discovery of biologically stable
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