LUF7982

Novel, selective A_2B covalent ligand (apparent pK_i values at A_2BARs are 8.10 and 9.17 (after 4h), where a K_i shift indicates a covalent mode of action). Displays ~100 -fold selectivity for A_2B compared to A₁, A_2A 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 A_2BAR.

Sold under license from the Oncode Institute and Universiteit Leiden

Novel Selective A_2B covalent ligand. Binds irreversibly.