Drug intelligence / Profile preview

pGlu(Lys8GluPAL)apelin-13 amide

Development stage
Unknown
Lead developer
Ulster University
Modality
Peptides, Small Molecules
Administration
Intraperitoneal
01

Overview

**pGlu(Lys8GluPAL)apelin-13 amide** is a chemically modified, long-acting fatty acid acylated analogue of the endogenous peptide apelin-13. This analogue is derivatized at the Lys^8^ residue with a palmitoylated glutamic acid (GluPAL) and N-terminal pyroglutamylation (pGlu), modifications which confer resistance to enzymatic degradation, extend circulating half-life, and enhance bioactivity compared to native apelin-13[5][8][3][1]. The compound acts as a **potent agonist of the apelin receptor (APJ)**, a G-protein-coupled receptor ubiquitously expressed in metabolic and cardiovascular tissues. In preclinical studies, pGlu(Lys8GluPAL)apelin-13 amide demonstrated robust insulinotropic effects, reduced food intake, decreased body weight, improved glucose tolerance, enhanced insulin sensitivity, lowered blood glucose, improved lipid profile, and reduced hepatic steatosis in high-fat diet and diabetic mouse models[1][3][5][8]. Its mechanism involves stimulating insulin secretion, improving glucose uptake in adipose and muscle tissue, and possibly preserving pancreatic islet cell morphology by reducing beta-cell apoptosis and transdifferentiation[1][3]. This analogue shows therapeutic promise for the treatment of **type 2 diabetes, obesity, and metabolic syndrome**[1][5][8].

Other names
pGlu(Lys8GluPAL)apelin-13 amidepGlu-apelin-13(Lys8GluPAL) amidepyroglutamyl-(Lys8GluPAL)-apelin-13 amide
02

Targets

APLNR (Apelin receptor)

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