Gue1654 is a Gβγ-signaling-biased 5-OxoETE receptor antagonist. It inhibits neutrophil and eosinophil shape change and chemotaxis induced by 5-OxoETE (Item No. 34250) but not chemoattractant C5a or prostaglandin D2 (PGD2; ). Gue1654 inhibits 5-OxoETE-induced Gβγ-mediated inositol monophosphate (IP1) production in HEK293 cells transiently expressing the 5-OxoETE receptor, an effect that can be blocked by the Gβγ-inhibitor gallein, but has no effect on IP1 production induced by stimulation of endogenous Gαq-linked muscarinic receptors. In a bioluminescence resonance energy transfer (BRET) assay, Gue1654 reduces the 5-OxoETE-induced, but not basal, BRET fluorescence response, indicating disruption of the interaction between ligand-activated 5-OxoETE receptor and Gβγ.
