CELT-327 hA2B/A3 Adenosine receptor fluorescent antagonist (589/616)

Our potent hA1/A2B Adenosine receptor fluorescent antagonist shows affinity for hA1and hA2B Adenosine receptors (Ki =1.89 nMand 24.65 nM respectively in radioligand binding assays), intermediate affinity for A2A (Ki=80.33 nM) and very low affinity for A3 Adenosine receptor (Ki =967.48 nM). 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.

Our potent and selective hA3 Adenosine receptor fluorescent antagonist shows high affinity for hA3 receptor and partial selectivity over the other receptor subtypes (Ki =52.7 nM for hA3 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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https://pubs.acs.org/doi/10.1021/acsmedchemlett.1c00598

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