Our GLP1R fluorescent antagonist shows high affinity for GLP1 receptor (pIC₅₀ = 7.2 for GLP1R) modulating the receptor by orthosteric antagonism. The efficacy and potency of LUXendin551 (CELT-111) as a GLP1R ligand was confirmed by inhibition of GLP-1-stimulated cAMP levels in SNAP-GLP1R: HEK293 cells. LUXendin551 (CELT-111) has been used in a variety of imaging applications, including widefield/confocal/2-photon microscopy in live and fixed mammalian cells and tissue, as well as anaesthetized mice.

*2º Image: Widefield image of live CHO-K1:SNAP-GLP1R cells labeled with 200 nM LUXendin551. Scale bar = 40 micrometer.

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https://chemrxiv.org/engage/chemrxiv/article-details/60ff0d5a393cc904c94f1f18