CELT-327

Key Product Details

Product Description

CELT-327 is a potent and selective fluorescent hA_2B/A₃ adenosine receptor antagonist (K_i values are 35.6 nM and 45.7 nM at A_2B and A₃ receptors respectively). It shows dose-dependent membrane fluorescent labeling in HCT116 cells expressing A_2B 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.

Scientific Data Images for CELT-327

Application of CELT-327 to live colorectal cancer cells.

HeLa cells were co-cultured with fibroblasts from the stroma around tumors (CAFs) previously labeled in green with a cell-tracker. Both cell types were incubated with CELT-327 (250 nM). The figure shows in red the plasma membrane staining revealed by CELT-327 specifically in HeLa cells.

Application of CELT-327 to fixed colorectal cancer cells.

HCT116 cells were fixed with PFA 4% (20 mins at room temperature) and then incubated with CELT-327 (250 nM) for 30 mins at room temperature, washed and visualized immediately (A), or 96h post-staining (B).

Licensing Information

Optical Data

Product Specifications for CELT-327

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Calculators

Background References

References are publications that support the biological activity of the product.

• Barbazán Identification of A_2BAR as a potential target in colorectal cancer using novel fluorescent GPCR ligands. Biomed.Pharmacother. 2022 PMID: 36076535

Product Documents for CELT-327