HTRF is a homogenous assay that combines fluorescence resonance energy transfer technology (FRET) with time-resolved measurement (TR). It is one of the most frequently used methodologies for drug target studies in high-throughput screening (HTS). In FRET assays, a signal is generated through fluorescent resonance energy transfer between a donor and an acceptor fluorophore when in close proximity one to each other.
FRET can be combined with TR measurements if lanthanides are used as donors, since they show long emission lifetimes allowing for a time delay of the signal detection between the excitation of the donor and the fluorescence of the acceptor fluorophore. For its unique features, in TR-FRET experiments, buffer and media interference is dramatically reduced. HTRF assay sensitivity and robustness make it appropriate for miniaturization in 384 and 1536-well plate formats.

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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 -
CELT-335 hCB1/CB2 Cannabinoids receptors fluorescent ligand (646/662)
10ug vial that allows to prepare 73ml of 100nM working solution to test CB1R/CB2R.
432,00€
Working concentration might differ among assay designsView moreOur CELT-335 product is a potent and selective hCB1/CB2 fluorescent ligand that shows a high affinity for CB1/CB2 receptors. It has a Ki value of 44.8 nM and 7.4 nM, respectively, in radioligand binding assay. CELT-335 has been validated in high-content screening assays and is also suitable for HTRF binding assays, providing a valid alternative to radioligand binding assays. It is available in a 10ug vial that allows for the preparation of 150ml of 100nM working solution to test CB1R/CB2R. CELT-335 is designed to allow for cell visualization in fluorescence microscopy and 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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If you want to know more about how to use fluorescent ligands to characterize receptors with pharmacological interest with this and other technologies, click on the button to download the article “Fluorescent ligands: A new method to label your GPCRs”