Especially, a TLR4 signaling inhibitor, TAK-242, could exert a protective effect on impairment in APP/PS1 transgenic AD mice, act as a microglia modulator, suppress MyD88/NF-κB/NLRP3 activation, and reverse microglial phenotype polarization from M1 to M2 in vitro and in vivo. This evidence concerns the gene TLR4 and Alzheimer disease.