Our GLP1R fluorescent antagonist shows high affinity for GLP1 receptor (pEC₅₀ = 7.5 for GLP1R) modulating the receptor by orthosteric antagonism. The efficacy and potency of LUXendin645 (CELT-112) as a GLP1R ligand was confirmed by inhibition of GLP-1-stimulated cAMP levels in SNAP-GLP1R:HEK293 cells. LUXendin645 (CELT-112) has been used in a variety of imaging applications, including widefield/confocal/2-photon microscopy in live and fixed mammalian cells and tissue. Using TR-FRET, LUXendin645 was used in GLP1R competitive binding experiments and in GLP1R trafficking and recycling studies.

*2º Image: Widefield image of live CHO-K1:SNAP-GLP1R cells labeled with 200 nM LUXendin645. Scale bar = 40 micrometer.

More information and applications

https://www.nature.com/articles/s41467-020-14309-w
https://pubmed.ncbi.nlm.nih.gov/34129856/
https://molpharm.aspetjournals.org/content/early/2021/07/27/molpharm.121.000270
https://pubs.acs.org/doi/10.1021/acsptsci.0c00022
https://www.sciencedirect.com/science/article/pii/S2452302X22001413?via%3Dihub