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Showing 1–15 of 28 results
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.
https://chemrxiv.org/engage/chemrxiv/article-details/60ff0d5a393cc904c94f1f18
Our GLP1R fluorescent antagonist shows high affinity for GLP1 receptor (pEC50 = 7.5 for GLP1R) modulating the rece
ptor 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.
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
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.
https://chemrxiv.org/engage/chemrxiv/article-details/60ff0d5a393cc904c94f1f18
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.
Our potent and partially selective 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 potent and partially selective hD3 Dopamine receptor fluorescent ligand shows 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.
https://www.frontiersin.org/articles/10.3389/fmolb.2023.1119157/full
Our potent 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.
Our potent hD2/D3 Dopamine receptors fluorescent ligand shows a high affinity for hD2 and hD3 receptors (Ki = 5.22 nM and 4.77 nM respectively in radioligand binding assays) nd 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.
Our potent and selective hD3 Dopamine receptors fluorescent ligand shows a high affinity for hD3 receptors (Ki = 75.4 nM in radioligand binding assays) and selectivity over D3 and 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.
Our potent and selective hA3 Adenosine receptor fluorescent antagonist shows high affinity and selectivity for hA3 receptor (Ki =12 nM for hA3 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.
Our potent C5a receptor fluorescent antagonist shows high affinity for the C5aR (EC50 = 24.89 nM by saturation binding in Chem1 transfected cells), good potency (KB= 5.8 μM by calcium flux assay) and good competition with the endogenous ligand C5a. It has been validated in flow cytometry competition binding assays using Chem1 transfected cells. It is potentially suitable for other fluorescence-based assays.
Our potent and selective hα1A adrenergic receptor fluorescent antagonist shows high affinity for α1A adrenergic receptor (Ki =28.3 nM measured in radioligand binding assay) and selectivity over α2A (Ki =1081 nM measured in radioligand binding assay). It is potentially suitable for fluorescence-based assays such as confocal microscopy or high content screening.
Our potent and selective hα1A adrenergic receptor fluorescent antagonist shows high affinity for alpha 1 adrenergic receptor (Ki =5 nM measured in radioligand binding assay) and selectivity over α2A (15% of displacement at 1 μM in radioligand binding assay). It is potentially suitable for fluorescence-based assays such as confocal microscopy, high content screening or fluorescence polarization.
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 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.