Glucagon-like peptide-1 receptor (GLP1R)

LUXendins have been developed by Johannes Broichhagen (Max Planck Institute for Medical Research, Heidelberg, Germany and Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany) and David J. Hodson (University of Birmingham). Celtarys has an exclusive worldwide licence for LUXendin commercialization.

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  • LUXendin551 glucagon-like peptide-1 receptor (GLP1R) fluorescent antagonist (551/576) (CELT-111)

    Our GLP1R fluorescent antagonist shows high affinity for glucagon-like peptide-1 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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  • LUXendin645 glucagon-like peptide-1 receptor (GLP1R) fluorescent antagonist (645/664) (CELT-112)

    Our GLP1R fluorescent antagonist shows high affinity for glucagon-like peptide-1 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.

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  • LUXendin762 glucagon-like peptide-1 receptor (GLP1R) fluorescent antagonist (762/784) (CELT-113)

    Our GLP1R fluorescent antagonist shows high affinity for glucagon-like peptide-1 receptor (pIC50 = 7.0 for GLP1R) modulating the receptor by orthosteric antagonism. The efficacy and potency of LUXendin762 (CELT-113) as a GLP1R ligand was confirmed by a GLP-1 stimulated cAMP levels in SNAP-GLP1R:HEK293 cells. LUXendin762 (CELT-113) has been used in a variety of imaging applications, including widefield imaging in live and fixed mammalian cells and tissue. LUXendin762 is also compatible with non-invasive fluorescence preclinical imaging.

    *2º Image: Widefield image of live CHO-K1:SNAP-GLP1R cells labeled with 200 nM LUXendin762. Scale bar = 40 micrometer.

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