LUF7746

The first covalent hA₁AR partial agonist which irreversibly activates the receptor (apparent pK_i values at CHO-hA₁ARs are 7.7 and 8.4 (after 4h), where a K_i shift indicates a covalent mode of action). Shown to covalently bind to the A₁AR receptor under many different experimental conditions. The Y271^7.36 tyrosine residue within the hA₁AR binding pocket has been demonstrated as the primary anchor point for this covalent interaction.

LUF7746 is a valuable probe for further mapping the receptor activation process.
Sold under license from the Oncode Cancer Institute and Universiteit Leiden

The first covalent hA₁AR partial agonist. Binds Irreversibly.