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Biological Activity:
Exenatide is an incretin mimic that acts as an agonist at the glucagon-like peptide 1 receptor to enhance insulin secretion in the presence of raised glucose concentrations. It is a 39-amino-acid peptide an insulin secretagogue with glucoregulatory effects. It displays biological properties similar to human glucagon-like peptide-1 (GLP-1), a regulator of glucose metabolism and insulin secretion. In contrast to DA-3091, which exhibited an HbA1c-lowering effect even at 0.1 mg/kg dose, the median effective exenatide dose [ED50] for Byetta® LAR was reported to be 74 μg, which approximately corresponded to an exenatide dose of 0.2 mg/kg.
References:
Pugazhenthi, U. et al.: Diabetol., 53, 2357 (2010); Li, C. et al.: Bioche,. Biophys. Res. Comm., 400, 563 (2010); Lupi, R. et al.: Diab. Obes. Metab., 10, 515 (2008); Kim, T.H. et al.: Bioconj. Chem., 22, 625 (2011).