TLR4 and colitis: In several colitis related studies, TAK-242 has been used as an antagonist to regulate TLR4 expression in vitro and in vivo, and the results showed that TAK-242 could block CYP3A4 and P-gp down-regulation induced by bacterial outer-membrane vesicles in Caco-2 cells and inhibit the phenotypic transition of Raw 264.7 macrophages [27, 28].