Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. It inhibits NO, TNF-α, and IL-6 production with IC50s of 1.8 nM, 1.9 nM, and 1.3 nM, respectively. This compound downregulates the expression of TLR4 downstream signaling molecules MyD88 and TRIF, inhibits autophagy, and plays a pivotal role in various inflammatory diseases.
- Selectively inhibits toll-like receptor 4 (TLR4).
- Inhibits nitric oxide (NO), TNF-α, and IL-6 production.
- Downregulates the expression of TLR4 downstream signaling molecules MyD88 and TRIF.
- Inhibits autophagy.
- Plays a pivotal role in various inflammatory diseases.
- Suppresses production from LPS-stimulated human peripheral blood mononuclear cells (PBMCs).
- Reverses LPS-induced body weight loss and muscle loss in mice models.