The first covalent hA1AR partial agonist which irreversibly activates the receptor (apparent pKi values at CHO-hA1ARs are 7.7 and 8.4 (after 4h), where a Ki shift indicates a covalent mode of action). Shown to covalently bind to the A1AR receptor under many different experimental conditions. The Y2717.36 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.