Resatorvid (TAK-242) is a selective inhibitor of Toll-like receptor 4 (TLR4). Resatorvid binds directly to Cys747 and prevents TLR4 from binding to TIRAP, thereby blocking downstream signaling. Resatorvid has antitumor activity, anti-inflammatory activity, and neuroprotective effects.

METHODS: Breast cancer cell lines MCF7, SKBR3, MDA-MB-231 and BT-474 were treated with Resatorvid (10-150 µM) for 48 h. Cell viability was measured using MTT Assay.
RESULTS: Resatorvid dose-dependently inhibited the viability of breast cancer cell lines. [1]
METHODS: Macrophage RAW264.7 was treated with Resatorvid (1-100 nM) and LPS (5 ng/mL), IFN-γ (1 U/mL) for 4 h. Gene expression levels were measured by RT-qPCR.
RESULTS: Resatorvid inhibited LPS and IFN-γ induced mRNA expression of IL-6 and TNF-α in RAW264.7 cells. [2]

METHODS: To test the effects on cancer-comorbid depression (BCCD), Resatorvid (3 mg/kg) was administered intraperitoneally to BALB/c mice in the BCCD model once daily for three weeks.
RESULTS: Resatorvid attenuated the symptoms of BCCD mice in vivo.Resatorvid inactivated inflammatory factors and TLR4/NF-κB/NLRP3 signaling pathway in vivo. [3]
METHODS: To investigate the effects on temporomandibular joint osteoarthritis (TMJOA), Resatorvid (10 mg/kg) was injected intraperitoneally twice weekly for four weeks into a CFA-induced TMJOA model in C57BL/6 mice.
RESULTS: Prophylactic treatment with Resatorvid attenuated TMJOA pathology by inhibiting chondrocyte focal prolapse and degeneration, and ROS-induced macrophage inflammation via TLR4/MyD88/NF-κB/NLRP3. [4]

Cell Line: RAW264.7 cells. Concentration: 1 nM, 10 nM, 100 nM. Incubation Time: 4 hours [1]

Animal Model: 30 ApoE knockout and 30 wild-type mice on a C57BL/6 background (female, 10 weeks old). Dosage: 0.3?mg/kg. Administration: i.p.; twice a week; for 4 weeks [3]