PSB-15160

PSB-15160 (compound 38) (preincubated for 5 min; Forskolin (HY-15371) 10 μM; additional 15 min) inhibits Forskolin-induced cAMP accumulation in a concentration-dependent manner in CHO cells stably expressing human GPR84, with an EC₅₀ of 80.0 nM and a maximum efficacy of 117% relative to the maximum effect of capric acid^[1].
PSB-15160 (preincubation for 5 min; Forskolin 10 μM; additional 15 min) inhibits cAMP accumulation in a concentration-dependent manner in CHO-hGPR84 cells, while no corresponding inhibitory effect is observed in parental CHO cells that do not express GPR84, indicating that this cAMP response is GPR84-dependent^[1].
PSB-15160 (90 min; 60 min additional incubation with detection reagent) induces β-arrestin recruitment in CHO-hGPR84 cells, with an EC₅₀ of 4.33 μM and a maximum efficacy of 125% relative to Embelin (HY-17473) (10 μM); its potency in the β-arrestin pathway is approximately 54-fold lower than that in the Gi/cAMP pathway, exhibiting a signaling profile biased toward Gi-mediated adenylate cyclase inhibition^[1].
PSB-15160 (10 μM) exhibits virtually no FFAR1 agonistic activity in the calcium mobilization assay using 1321N1 astrocytoma cells recombinantly expressing human FFAR1^[1].
PSB-15160 (10 μM; 90 min in agonist assay; additional 60 min for detection) exhibits essentially no agonistic activity in CHO cells recombinantly expressing human FFAR4; after pre-incubation for 30 min prior to the addition of TUG-891 (HY-100881) (4 μM) in an agonist screening assay, PSB-15160 shows no FFAR4 inhibition^[1].
PSB-15160 (10 μM) exhibits no agonistic activity at human GPR35, a phylogenetically related receptor of the GPR84 system^[1].
PSB-15160 (5, 20 μM; 18 h) only weakly induces the expression of the AhR target gene CYP1A1 in HepG2 cells at 20 μM, and its effect is significantly weaker than that of the lead compound 1; accordingly, the AhR activity of PSB-15160 is markedly reduced relative to its GPR84 agonistic activity^[1].

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