Abstract: G protein-coupled receptor (TGR5) is a cell-surface bile acid receptor which is closely related to glucose metabolism, energy expenditure and the secretion of glucagons-like peptide-1. TGR5 is a potential target for diagnosis, treatment and prognosis evaluation of the tumors, whose expression is strongly upregulated in many tumors compared to expression levels in normal tissues and is associated with the prognosis of the patients. Therefore, the ¹⁸F-PET probe ［¹⁸F］FEA-LCA was prepared with the simply and efficiency click chemistry method with a high radiochemical yield (66%-74%), high radiochemical purity (>99%), and high specific activity (>300 PBq/mol). ［¹⁸F］FEA-LCA has a similar lipophilicity to the parental bile acid lithocholic acid and a high metabolic stability in vitro. This work make a solid foundation for further study the ［¹⁸F］FEA-LCA as the PET probe to the tumors of TGR5-overexpression.