Novel, selective A2B covalent ligand (apparent pKi values at A2BARs are 8.10 and 9.17 (after 4h), where a Ki shift indicates a covalent mode of action). Displays ~100 -fold selectivity for A2B compared to A1, A2A and A3 receptors. LUF7982 covalently targets lysine residue(s) on the receptor and binds persistently in radioligand displacement and wash-out assays. LUF7982 allows for novel ways to interrogate the A2BAR.
Sold under license from the Oncode Institute and Universiteit Leiden