GLP-1R agonist 30 is a highly selective and orally active agonist of the glucagon-like peptide-1 receptor (GLP-1R), demonstrating an EC50 of 0.048 nM. It displays significant selectivity with EC50 values greater than 20 μM for GLP-2 receptor, GIP receptor, and glucagon receptor. This compound enhances cAMP signaling while minimizing hERG inhibition, indicating favorable safety profiles. It effectively improves glucose tolerance and promotes insulin secretion in B-hGLP1R knock-in mouse models, making it a valuable tool for research applications in diabetes and metabolic disorders.
GLP-1R agonist 30 is a highly selective and orally active agonist of the glucagon-like peptide-1 receptor (GLP-1R), demonstrating an EC50 of 0.048 nM. It displays significant selectivity with EC50 values greater than 20 μM for GLP-2 receptor, GIP receptor, and glucagon receptor. This compound enhances cAMP signaling while minimizing hERG inhibition, indicating favorable safety profiles. It effectively improves glucose tolerance and promotes insulin secretion in B-hGLP1R knock-in mouse models, making it a valuable tool for research applications in diabetes and metabolic disorders.
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