Our proprietary technology enables the synthesis of fluorescent ligands with exceptional performance features, including high potency, selectivity, and affinity. Our ligands have been designed to fill the gaps in the available tools for HTS, making the screening process faster and more efficient than ever before.
This technology has been used to study a variety of signaling pathways in drug discovery, providing an invaluable resource for researchers interested in GPCR signaling and drug discovery.
At Celtarys, we are committed to providing you with the best products on the market for GPCR research and drug discovery, and we are constantly developing new solutions to meet your needs.
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Showing 1–15 of 33 results
Our CELT-011 fluorescent antagonist has a high affinity for h5HT2A/h5HT2C serotonin receptors (Ki =48.8 nM and 28.8 nM, respectively in radioligand binding assay). With a 10ug vial that allows you to prepare 80ml of 100nM working solution, this product is perfect for testing 5HT2AR/5HT2CR. It enables cell visualization in fluorescence microscopy, confocal microscopy, and high-content system experiments, and it is potentially suitable for other fluorescence-based assays, such as fluorescence polarization.
Our CELT-145 ligand is a highly potent fluorescent antagonist developed for hA1R testing with a Ki of 160 nM in radioligand binding assay. The product comes in a 10ug vial that enables the preparation of 63ml of 100nM working solution to test AT1R. Our fluorescent antagonist is ideal for visualization in confocal microscopy and high-content system experiments. Our CELT-145 ligand is potentially suitable for other fluorescence-based assays such as HTRF.
Our CELT-252 ligand is a highly potent fluorescent antagonist developed for hA1R testing with a Ki of 39 nM in radioligand binding assay. The product comes in a 10ug vial that enables the preparation of 69ml of 100nM working solution to test AT1R. Our fluorescent antagonist is ideal for visualization in confocal microscopy and high-content system experiments. Our CELT-252 ligand is potentially suitable for other fluorescence-based assays such as Fluorescence Polarization.
Our potent CELT-150 VHL E3 ligase fluorescent ligand is a tracer for VHL E3 ligases binding assays, designed to perform affinity binding curves to VHL protein using TR-FRET homogenous technology.
Von Hippel–Lindau protein (VHL) is the substrate recognition subunit of an E3 ligase recruited by bifunctional Proteolysis-targeting chimeras (PROTACs) to induce ubiquitination and subsequent proteasomal degradation of a targeted protein.
Our CELT-249 ligand is a highly potent fluorescent antagonist developed for hM1R and hM2R testing with a Ki of 133 nM and 11.5 nM, respectively in radioligand binding assay. The product comes in a 10ug vial that enables the preparation of 82ml of 100nM working solution to test M1R/M2R. Our fluorescent antagonist is ideal for visualization in confocal microscopy and high-content system experiments. Our CELT-249 ligand is potentially suitable for other fluorescence-based assays
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 hD3 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.