CELT-448 hA1 Adenosine receptor fluorescent antagonist (560/571)

Our potent and partially selective hA1 Adenosine receptor fluorescent antagonist shows higher affinity for hA1 (Ki =8.60 nM) compared to hA2A, hA2B and hA3 Adenosine receptors (Ki= 98.38 nM, 72.24 and 231.01 nM respectively in 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.

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.