AP-7-168, molecular glues, is a β-arrestin-biased negative allosteric modulator of the β2-adrenergic receptor ( β2AR ). AP-7-168 can promote β2AR homodimerization and inhibit GRK5-mediated β2AR phosphorylation. AP-7-168 can sustain bronchorelaxation in cell and tissue. AP-7-168 can be used for the researches of inflammation and immunology, such as asthma [1].
In Vitro, AP-7-168 (0.03-100 μM, 1 h) promotes β2AR homodimerization in HEK293 cells with a pEC50 of 5.93[1]. AP-7-168 (10 μM) inhibits β-arrestin2 recruitment and GRK5-mediated β2AR phosphorylation in β2AR-expressing cells[1].
References:
[1]. Jiemin Shen, et al. A biased allosteric modulator functions as a molecular glue to induce β2AR dimerization. bioRxiv. October 22, 2025.
In Vitro, AP-7-168 (0.03-100 μM, 1 h) promotes β2AR homodimerization in HEK293 cells with a pEC50 of 5.93[1]. AP-7-168 (10 μM) inhibits β-arrestin2 recruitment and GRK5-mediated β2AR phosphorylation in β2AR-expressing cells[1].
References:
[1]. Jiemin Shen, et al. A biased allosteric modulator functions as a molecular glue to induce β2AR dimerization. bioRxiv. October 22, 2025.