Products
Our GPCR fluorescent ligands have been designed to fill current gaps in the available tools ready to use in HTS.
Applying our proprietary synthetic technology we can satisfy the demands of big collaborative or corporative projects that need high quantities of fluorescent ligands.
Our ligands’ value:
- Potent (Ki < 100 nM) and subtype selective ( > 100-fold). Their high affinity allows to perform thousands of test in HTS assays (typically 3.000-6.000 points in 384 plates for a 10µg vial).
- Their fluorophores are stable, guarantee their affinity and display a variety of photo-physical properties that meet the market demand for several applications from competitive binding assays to microscopy
- Their pharmacophores are representative of the target and aligned with international standards
- Their spacers allow optimal target recognition and placing of the fluorophore in the outer region of the membrane.
Published articles using our fluorescent probes
CELT-228 hA3 Adenosine receptor fluorescent antagonist (560/671)
CELT-335 hCB1/CB2 Cannabinoids receptors fluorescent ligand (646/662)
CELT-327 hA2B/A3 Adenosine receptor fluorescent antagonist (589/616)
LUXendin 551 glucagon-like peptide-1 receptor (GLP1R) fluorescent antagonist (551/576) (CELT-111)
LUXendin 645 glucagon-like peptide-1 receptor (GLP1R) fluorescent antagonist (645/664) (CELT-112)
LUXendin 762 glucagon-like peptide-1 receptor (GLP1R) fluorescent antagonist (762/784) (CELT-113)
CELT-419 hD3 Dopamine receptor fluorescent ligand (560/571)
Do you want more information?
We are ready to support your challenges
Showing 1–15 of 28 results
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LUXendin551 GLP1 receptor (GLP1R) fluorescent antagonist (551/576) (CELT-111)
3nmoles vial that allows to prepare 30ml of 100nM working solution to test GLP1R. One vial is sufficient for injecting one mouse.
385,00€
Working concentration might differ among assay designs.View moreOur 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)
3nmoles vial that allows to prepare 30ml of 100nM working solution to test GLP1R. One vial is sufficient for injecting one mouse.
385,00€
Working concentration might differ among assay designs.View moreOur 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.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 -
LUXendin762 GLP1 receptor (GLP1R) fluorescent antagonist (762/784) (CELT-113)
3nmoles vial that allows to prepare 30ml of 100nM working solution to test GLP1R. One vial is sufficient for injecting one mouse.
385,00€
Working concentration might differ among assay designs.View moreOur 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)
10ug vial that allows to prepare 3400ml of 100nM working solution to test D2R.
432,00€
Working concentration might differ among assay designsView moreOur 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- 426 hD2 Dopamine receptor fluorescent antagonist (560/571)
10ug vial that allows to prepare 37ml of 100nM working solution to test D2R.
432,00€
Working concentration might differ among assay designsView moreOur 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.
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CELT- 419 hD3 Dopamine receptor fluorescent ligand (560/571)
10ug vial that allows to prepare 55ml of 100nM working solution to test D3R.
432,00€
Working concentration might differ among assay designsView moreOur 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.
More information and applications
https://www.frontiersin.org/articles/10.3389/fmolb.2023.1119157/full
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CELT-240 hD2/D3 Dopamine receptors fluorescent ligand (589/616)
10ug vial that allows to prepare 1700ml of 100nM working solution to test D2R/D3R.
432,00€
Working concentration might differ among assay designsView moreOur 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.
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CELT-241 hD2/D3 Dopamine receptors fluorescent ligand (646/662)
10ug vial that allows to prepare 680ml of 100nM working solution to test D2R/D3R.
432,00€
Working concentration might differ among assay designsView moreOur 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.
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CELT-429 hD3 Dopamine receptor fluorescent ligand (589/616)
10ug vial that allows to prepare 50ml of 100nM working solution to test D3R.
432,00€
Working concentration might differ among assay designsView moreOur 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.
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CELT- 480 hA3 Adenosine receptor fluorescent antagonist (646/662)
10ug vial that allows to prepare 290ml of 100nM working solution to test A3R.
432,00€
Working concentration might differ among assay designsView moreOur 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.
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CELT- 58 C5a receptor fluorescent antagonist (646/662)
10ug vial that allows to prepare 175ml of 100nM working solution to test C5aR.
432,00€
Working concentration might differ among assay designs.View moreOur 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.
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CELT-130 hα1 adrenergic receptor fluorescent antagonist (646/662)
10ug vial that allows to prepare 150ml of 100nM working solution to test alpha1AR.
432,00€
Working concentration might differ among assay designsView moreOur 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.
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CELT-133 hα1 adrenergic receptor fluorescent antagonist (560/571)
10ug vial that allows to prepare 830ml of 100nM working solution to test alpha1AR.
432,00€
Working concentration might differ among assay designsView moreOur 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.
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CELT-175 hD2 Dopamine receptor fluorescent antagonist (748/776)
10ug vial that allows to prepare 1000ml of 100nM working solution to test D2R.
432,00€
Working concentration might differ among assay designsView moreOur 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.
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CELT-298 Pan Adenosine receptors fluorescent antagonist (646/662)
10ug vial that allows to prepare 65ml of 100nM working solution to test A2AR.
432,00€
Working concentration might differ among assay designsView moreOur 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.