GPR34 agonist 1

GPR34 agonist 1 (0.1-100 nM; 1.5-7.5 h) specifically enhances fibrillar Aβ uptake by mouse primary microglia in a concentration- and time-dependent manner, with an EC₅₀ of 5 nM, without affecting uptake of soluble Aβ species or other phagocytic substrates^[1].
GPR34 agonist 1 (10 nM) reduces intracellular cAMP levels in mouse primary microglia, which reverses forskolin-mediated suppression of fibrillar Aβ uptake^[1].
GPR34 agonist 1 (10-100 nM; 4.5 h) enhances fibrillar Aβ uptake by human iPSC-derived microglia-like cells, with significant activity at 100 nM^[1].
GPR34 agonist 1 potently activates human GPR34 expressed in HEK293A cells, with key interactions mediated by hydrophilic pocket residues and the L-shaped hydrophobic pocket formed by L223⁵·^43[2].
GPR34 agonist 1 (1-10 μM; overnight) binds to human GPR34 in a stable conformation, engaging both hydrophilic and hydrophobic binding pockets, and forms a high-resolution GPR34-G_i complex suitable for structural analysis^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.