Labelling

Our hD3 Dopamine receptor fluorescent ligandshows high affinity for hD2 receptor and partial selectivity over the other receptor subtypes (Ki =65.6 nM for hD3 receptor in radioligand binding assay). It has been validated in Fluorescence Polarization binding assays as a valid alternative to 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.

Our hD2 Dopamine receptor fluorescent antagonist shows high affinity for hD2 receptor and partial selectivity over the other receptor subtypes (Ki =89.3 nM for hD2 receptor in radioligand binding assay). It has been validated in Fluorescence Polarization binding assays as a valid alternative to 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.

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.

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.

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.

Our potent and selective hD2 Dopamine receptor fluorescent antagonist shows high affinity for hD2 receptor and selectivity over the other receptor subtypes (Ki =3.15 nM for hD2 receptor and Ki =294.6 nM and Ki =220.3 nM for D3 and D4 receptor, 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.

Our hM1 Muscarinic receptor fluorescent antagonist shows high affinity for M1 Muscrinic receptor (Ki =57.77 nM in radioligand binding assay). It allows to perform cell visualization in confocal microscopy and high content system experiments as a valid alternative to radioligand binding assays. It is potentially suitable for other fluorescence-based assays.

Our hA3 Adenosine receptor fluorescent antagonist shows high affinity for hA3 receptor and partial selectivity over the other receptor subtypes (Ki =52.7 nM for hA3 receptor in radioligand binding assay). It has been validated in Fluorescence Polarization binding assays as a valid alternative to 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.

Our hD3/D2 Dopamine receptors fluorescent ligand shows high affinity for hD2 and hD3 receptors (Ki =2.34 nM and 2.14 nM respectively in radioligand binding assays) and selectivity over D4 dopamine receptor. 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.