NNC-0640

NNC-0640 (CAS No.: 307986-98-7) is a potent negative allosteric modulator of the human glucagon receptor (GCGR), a class B G protein-coupled receptor that plays a central role in glucose homeostasis through regulation of hepatic glucose production and metabolic signaling pathways. By binding to an allosteric site distinct from the endogenous ligand-binding domain, NNC-0640 attenuates receptor activation and downstream signaling, including cyclic AMP production, thereby modulating glucagon-mediated metabolic effects. It exhibits inhibitory activity in the nanomolar range, with reported IC50 and binding affinity values indicating high potency toward GCGR. This compound is widely used as a pharmacological tool in biochemical and cellular studies to investigate glucagon receptor function, receptor conformational dynamics, and GPCR allosteric modulation mechanisms. In drug discovery, NNC-0640 serves as a reference molecule for the development of novel therapeutics targeting metabolic disorders such as diabetes and obesity. Experimental applications typically include receptor binding assays, signal transduction studies, and metabolic profiling in relevant cell-based systems or preclinical models, with concentrations adjusted according to specific assay requirements and study objectives.