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DL-175 is a potent and selective biased GPR84 agonist with EC50 of 33 nM.DL-175 exhibits no significant activity in a panel of 168 other GPCRs.DL-175 display significantly biased signaling across GPR84-overexpressing cells, primary murine macrophages, and human U937 cells.DL-175 markedly different abilities to induce chemotaxis in human myeloid cells, while causing similar levels of phagocytosis enhancement.
PSB-16671 is a novel orthosteric and allosteric activator of GPR84, activates human GPR84 with EC50 of 41.3 nM in cAMP accumulation assays.
PSB-16671 is selective versus related fatty acid receptors and the arylhydrocarbon receptor.
PSB-16671 shows an EC50 of 5.47 uM in β-Arrestin assays, and allosteric KB value of 634 nM.
TUG-2181 is an antagonist of GPR84 with an IC50 value of 34 nM. TUG-2181 inhibits GPR84 agonists-induced reactive species oxygen (ROS) production and IL-8 release in human neutrophils. TUG-2181 can be used for inflammation and fibrosis study.
OX04529 is a highly potent, selective, G-protein pathway biased and orally bioavailable GPR84 agonist with EC50 of 18.5 pM for inhibition of FSK (25 uM)-induced cAMP production in CHO-hGPR84 cells.
OX04528 is a highly potent, selective, G-protein pathway biased and orally bioavailable GPR84 agonist with EC50 of 5.98 pM for inhibition of FSK (25 uM)-induced cAMP production in CHO-hGPR84 cells.
PBI-4547 is an agonist of GPR40/120 and an antagonist of GPR84, also is a partial ligand and activator of PPAR.PBI-4547 dose-dependently inhibits GPR84/Gαi2 activation (reflected by an increase in BRET signal) with IC50 of 17 uM, activates GPR40 (EC50 of 102 µM for Gαq and 16 µM for Gαi2) and dose-dependently promoted β-arrestin-2 recruitment to GPR120 (EC50=148 uM).PBI-4547 prevents progression, improves glucose metabolism in a mouse model of NAFLD, restores hepatic glucose and FA metabolism.
DL-175 is a potent and selective biased GPR84 agonist with EC50 of 33 nM.DL-175 exhibits no significant activity in a panel of 168 other GPCRs.DL-175 display significantly biased signaling across GPR84-overexpressing cells, primary murine macrophages, and human U937 cells.DL-175 markedly different abilities to induce chemotaxis in human myeloid cells, while causing similar levels of phagocytosis enhancement.
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