Catalog No.: PC-27918Not For Human Use, Lab Use Only.
AP-7-168 is a specific β-arrestin-biased negative allosteric modulator (NAM) of β2-adrenergic receptor (β2AR), mediates β2AR dimerization with pEC50 of 5.93 in HEK cells, is >1,000-fold effective at inhibiting β-arrestin2 recruitment versus cAMP production.
AP-7-168 is a specific β-arrestin-biased negative allosteric modulator (NAM) of β2-adrenergic receptor (β2AR), mediates β2AR dimerization with pEC50 of 5.93 in HEK cells, is >1,000-fold effective at inhibiting β-arrestin2 recruitment versus cAMP production.
AP-7-168 shows direct binding to the monomeric β2AR receptor with Kd of 30 uM.
AP-7-168 promotes β2AR dimerization in continuous membranes and in cells.
AP-7-168 (10 uM) caused a slight reduction in the monomer–Gs binding affinity (KD = 1.7 μM) in BLI assays.
AP-7-168 biases TM6 conformational dynamics of β2AR in both dimer and monomer.
AP-7-168-bound β AR dimers inhibits GRK5-mediated phosphorylation of β2AR in both detergent and nanodiscs.
