Fluorescence Microscopy

Our fluorescent ligands have been extensively validated as useful tools to visualize GPCRs in native and transfected cells, both in living cells and in cells after fixation.

Celtarys Ligands validated for Fluorescence Microscopy assays
  • LUXendin551 GLP1 receptor (GLP1R) fluorescent antagonist (551/576) (CELT-111)

    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.

    More information and applications

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

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  • LUXendin645 GLP1 receptor (GLP1R) fluorescent antagonist (645/664) (CELT-112)

    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

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  • LUXendin762 GLP1 receptor (GLP1R) fluorescent antagonist (762/784) (CELT-113)

    Our GLP1R fluorescent antagonist shows high affinity for GLP1 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.

    More information and applications

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

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  • CELT- 174 hD2 Dopamine receptor fluorescent antagonist (589/616)

    Our potent and selective hD2 Dopamine receptor fluorescent antagonist shows high affinity for hD2 receptor and selectivity over the other receptor subtypes (Ki =1.06 nM for hD2 receptor in radioligand binding assay). It allows to perform cell visualization in fluorescence microscopy, confocal microscopy and high content system experiments. It is potentially suitable for other fluorescence-based assays.

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  • CELT-298 Pan Adenosine receptors fluorescent antagonist (646/662)

    Our potent Pan Adenosine receptors fluorescent antagonist shows affinity for hA1, hA2A, hA2B and hA3 Adenosine receptors (Ki =20.9 nM, 171 nM, 44,7nM and 95.2 nM respectively in radioligand binding assays). It allows to perform cell visualization in fluorescence microscopy, confocal microscopy and high content system experiments. It is potentially suitable for other fluorescence-based assays.

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  • CELT-360 hA1 Adenosine receptor fluorescent antagonist (646/662)

    Our potent and partially selective hA1 Adenosine receptor fluorescent antagonist shows higher affinity for hA1 (Ki =8.60 nM) compared to hA2A, hA2B and hA3 Adenosine receptors (Ki= 98.38 nM, 72.24 and 231.01 nM respectively in radioligand binding assays). It allows to perform cell visualization in fluorescence microscopy, confocal microscopy and high content system experiments. It is potentially suitable for other fluorescence-based assays.

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  • CELT-327 hA2B/A3 Adenosine receptor fluorescent antagonist (589/616)

    Our potent hA2B/A3 Adenosine receptor fluorescent antagonist shows high affinity for hA2B and A3 receptor (Ki =35.6 nM and 45.7 nM respectively in radioligand binding assay). It allows to perform cell visualization in fluorescence microscopy, confocal microscopy and high content system experiments. It is potentially suitable for other fluorescence-based assays.

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  • CELT- 171 hA3 Adenosine receptor fluorescent antagonist (589/616)

    Our potent and selective hA3 Adenosine receptor fluorescent antagonist shows a high affinity and selectivity for hA3 receptor over the other receptor subtypes (Ki =6.13 nM for A3 receptor in radioligand binding assay). It allows to perform cell visualization in fluorescence microscopy, confocal microscopy and high content system experiments. It is potentially suitable for other fluorescence-based assays.

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  • CELT- 211 h5HT2B Serotonin receptor fluorescent ligand (589/616)

    Our potent and selective h5HT2B Serotonin receptor fluorescent ligand shows a high affinity for 5HT2B serotonin receptor and high selectivity over the other receptor subtypes (Ki =56.32 nM for 5HT2B receptor in radioligand binding assay).It allows to perform cell visualization in fluorescence microscopy, confocal microscopy and high content system experiments. It is potentially suitable for other fluorescence-based assays.

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  • CELT-335 hCB1/CB2 Cannabinoids receptors fluorescent ligand (646/662)

    Our potent hCB cannabinoids receptors fluorescent ligand shows high affinity for hCB1/CB2 cannabinoids receptor (Ki =44.8 nM and 7.4 nM , respectively in radioligand binding assay). It has been validated in High Content Screening assays and it is suitable also for HTRF binding assays as a valid alternative to radioligand binding assays. It allows to perform cell visualization in fluorescence microscopy and it is potentially suitable for other fluorescence-based assays.

    More information and applications

    https://www.sciencedirect.com/science/article/pii/S1043661821005545?via%3Dihub

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  • CELT-331 hCB2 Cannabinoids receptor fluorescent ligand (646/662)

    Our potent and selective hCB2 cannabinoids receptor fluorescent ligand shows high affinity for hCB2 cannabinoids receptor and selectivity over hCB1 (Ki =75.9 nM for hCB2 receptor in radioligand binding assay). It is suitable for HTRF binding assays as a valid alternative to radioligand binding assays. It allows to perform cell visualization in fluorescence microscopy, confocal and high content system experiments. It is potentially suitable for other fluorescence-based assays.

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