Tocris Bioscience™ CELT-327

CELT-327 is a potent and selective fluorescent hA2B/A3 adenosine receptor antagonist (Ki values are 35.6 nM and 45.7 nM at A2B and A3 receptors respectively). It shows dose-dependent membrane fluorescent labeling in HCT116 cells expressing A2B adenosine receptors, with rapid diffusion and homogeneous distribution of the fluorescence signal within the cell monolayer. In live HCT116 compact spheroids, CELT-327 displays homogeneous staining across the entire spheroid diameter, reaching deep spheroid regions. CELT-327 can be used as a fluorescent adenosine receptor probe for fluorescence binding assays, live cell imaging, flow cytometry, and fluorescence polarization assays. It is a suitable replacement for GPCR radiolabeling ligands. Excitation and emission maxima (λ) are 589 nm and 616 nm, respectively. Wavelengths are compatible with use as an acceptor dye in TR-FRET assays, together with the CoraFluor™ 1 (Cat. No. 7920) TR-FRET donor. Add 75 μL of assay buffer containing 1% of DMSO to obtain a 100 μM stock solution, and use 250 nM as a working concentration.