Exendin-4£¬IC-0324402

Glucagon-like peptide-1 (GLP-1) is an enteroendocrine hormone that has a capacity, when administered exogenously, to normalize blood glucose levels in type 2 diabetes mellitus. Exendin-4, a 39-amino acid (AA) peptide, is a long-acting agonist at the GLP-1 receptor with an IC₅₀ value of 3.22 nM^[3]. In human umbilical vein endothelial cells (HUVECs), exendin-4 significantly increased NO production, endothelial NO synthase (eNOS) phosphorylation, and GTP cyclohydrolase 1 (GTPCH1) level in a dose-dependent manner^[4]. In vivo, ob/ob mice sustained a reduction in the net weight gained during exendin-4 treatment (10 ¦Ìg/kg or 20 ¦Ìg/kg for 60 days). Furthermore, serum glucose and hepatic steatosis was significantly reduced and insulin sensitivity was improved in exendin-4 treated ob/ob mice^[5].

[1]Tsutsumi Y, Nomiyama T, et al. Combined Treatment with Exendin-4 and Metformin Attenuates Prostate Cancer Growth. PLoS One. 2015 Oct 6;10(10):e0139709.