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Description: Potent and selective hA2B/A3 adenosine receptor fluorescent antagonist
Purity: ≥95% (HPLC)
Literature (2)

Biological Activity for 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.

Scientific Data

Live-cell Imaging Application of CELT-327 to live colorectal cancer cells View Larger

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.

Fixed-cell Imaging Application of CELT-327 to fixed colorectal cancer cells. View Larger

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

Sold under license from Celtarys Research

Optical Data for CELT-327

Emission Color Orange
λabs 589 nm
λem 616 nm
Closest Laser line 561 nm
Application Confocal microscopy, High-content screening

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Technical Data for CELT-327

M. Wt 1334.19
Storage Store at -20°C
Purity ≥95% (HPLC)

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

References for CELT-327

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

Barbazán et al (2022) Identification of A2BAR as a potential target in colorectal cancer using novel fluorescent GPCR ligands. Biomed.Pharmacother. 153 113408 PMID: 36076535

If you know of a relevant reference for CELT-327, please let us know.

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Citations for CELT-327

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Fluorescent Dyes and Probes Research Product Guide

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Enabling Research By Provision of Chemical Tools Poster

Enabling Research By Provision of Chemical Tools Poster

The Tocris chemistry team has considerable chemistry knowledge and skill which it has recently been applying to the generation of new chemical probes from known tools and compounds to help answer biological questions. This poster presents some of the work carried out by Tocris scientists and focuses on two areas: the generation of libraries of chemical building blocks to support Degrader (PROTAC) research and the development of a fluorescent probe to study integrin biology. Presented at Chemical Tools for Complex Biological Systems II, 2019, Janelia Research Campus, USA.