Exendin-4 Acetate

Exendin-4 Acetate, a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM.

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

10 mM in H₂O

Glucagon Receptor

In human umbilical vein endothelial cells, exendin-4 significantly increases NO production, endothelial NO synthase (eNOS) phosphorylation, and GTP cyclohydrolase 1 (GTPCH1) level in a dose-dependent manner. Exendin-4 shows cytotoxic effects to MCF-7 breast cancer cells with IC50 of 5 μM at 48 hour.

Both low- and high-dose exendin-4 treatment in ob/ob mice improve serum ALT and reduce serum glucose, insulin levels and calculated HOMA scores compared with control. Exendin-4-treated ob/ob mice sustain a marked reduction in the net weight gain in the final 4 weeks of the study period. Animals treated with exendin-4 have more pancreatic acinar inflammation, more pyknotic nuclei and weigh significantly less than control rats. Exendin-4 treatment is associated with lower insulin and leptin levels as well as lower HOMA values in rats. Exenatide causes dose-dependent relaxation of rat thoracic aorta, which is evoked via the GLP-1 receptor and is mediated mainly by H2S but also by NO and CO.

[1]. Lital Rachmany, et al. Exendin-4 induced glucagon-like peptide-1 receptor activation reverses behavioral impairments of mild traumatic brain injury in mice. AGE.October 2013, Volume 35, Issue 5, pp 1621-1636.



[2]. Arakawa M, et al. Inhibition of Monocyte Adhesion to Endothelial Cells and Attenuation of Atherosclerotic Lesion by a Glucagon-like Peptide-1 Receptor Agonist, Exendin-4. Diabetes. 2010 Apr;59(4):1030-7.



[3]. Erdogdu O, et al. Exendin-4 stimulates proliferation of human coronary artery endothelial cells through eNOS-, PKA- and PI3K/Akt-dependent pathways and requires GLP-1 receptor. Molecular and Cellular Endocrinology.2010, 325(1-2):26-35.



[4]. Al-Barazanji KA, et al. Central Exendin-4 Infusion Reduces Body Weight without Altering Plasma Leptin in (fa/fa) Zucker Rats. Obesity Research. 2000,8 (4): 317-323.