Drug intelligence / Profile preview

pyroglutamated apelin-13

Development stage
Unknown
Lead developer
Imperial College London
Modality
Peptides
Administration
Intra-arterial, Intravenous
01

Overview

Pyroglutamated apelin-13 ([Pyr1]apelin-13) is a naturally occurring, post-translationally modified peptide and the predominant circulating isoform of apelin in human plasma and cardiovascular tissues. It acts as a potent agonist of the apelin receptor (APJ), a G protein-coupled receptor that regulates cardiovascular homeostasis, vascular tone, and fluid balance. The N-terminal pyroglutamate modification enhances the peptide's stability and resistance to enzymatic degradation compared to unmodified apelin-13, though it still retains a short in vivo half-life of only a few minutes. Pyroglutamated apelin-13 has been investigated in early-phase clinical trials for its vasodilatory, inotropic, and aquaretic properties in conditions such as chronic kidney disease, heart failure, pulmonary arterial hypertension, and the syndrome of inappropriate antidiuresis (SIAD).

Other names
(Glp1)-Apelin-13(pGlu1)apelin-13(Pyr1)apelin-135-oxo-L-prolyl-L-arginyl-L-prolyl-L-arginyl-L-leucyl-L-seryl-L-histidyl-L-lysylglycyl-L-prolyl-L-methionyl-L-prolyl-L-phenylalaninep-Glu-Arg-Pro-Arg-Leu-Ser-His-Lys-Gly-Pro-Met-Pro-PhePyr-apelin-13Pyr-apelin13Pyr-apelin 13Pyr1-apelin-13Pyr-1-apelin-13Pyr 1-apelin-13pyroglutaminated apelin-13pyroglutamyl apelin-13[pGlu1]-apelin-13[Pyr1]-apelin-13[Pyr1]apelin-13
02

Targets

APLNR (Apelin receptor)

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