| Name | Resatorvid |
| Description | Resatorvid (TAK-242), a selective Toll-like receptor 4 (TLR4) inhibitor, binds directly to Cys747 to prevent TLR4-TIRAP interaction, thereby blocking downstream signaling. Resatorvid exhibits antitumor, anti-inflammatory, and neuroprotective activities. |
| Cell Research | Cell Line: RAW264.7 cells. Concentration: 1 nM, 10 nM, 100 nM. Incubation Time: 4 hours [1] |
| Animal Research | 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] |
| In vitro | 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] |
| In vivo | 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] |
| Storage | keep away from direct sunlight,store at low temperature | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (13.82 mM), Sonication is recommended.
H2O : Insoluble
DMSO : 255 mg/mL (704.77 mM), Sonication is recommended.
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| Keywords | Tumor Necrosis Factor Receptor | TRIF | Toll-like Receptor (TLR) | TNF-R | TNFR | TNF Receptor | TLR4 | TLR | TAK242 | TAK 242 | Resatorvid | MyD88 | Interleukin Related | Interleukin | Inhibitor | inhibit | inflammatory | IL-6 | diseases | CLI095 | CLI 095 | Autophagy |
| Inhibitors Related | Kaolin | Stavudine | Aceglutamide | Hemin | D(+)-Raffinose pentahydrate | Guanidine hydrochloride | Hydroxychloroquine | Hydroxypropyl Cellulose | Paeonol | Naringin | Gluconate Calcium | Alginic acid |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Neuroprotective Compound Library | Inhibitor Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
