Resatorvid [243984-11-4]
Référence TQ0181-10mg
Conditionnement : 10mg
Marque : TargetMol
Resatorvid (Synonyms: TAK-242, CLI-095)
Resatorvid
Copy Product InfoSynonyms TAK-242, CLI-095
Cas No. 243984-11-4
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.9%
Color:White
COA HNMR HPLC
Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| 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. |
| Targets&IC50 | IL-6:1.3 nM, NO:1.8 nM, TNF R:1.9 nM |
| 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] |
| 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] |
| Synonyms | TAK-242, CLI-095 |
| Molecular Weight | 361.82 |
| Formula | C15H17ClFNO4S |
| Cas No. | 243984-11-4 |
| Smiles | CCOC(=O)C1=CCCC[C@H]1S(=O)(=O)Nc1ccc(F)cc1Cl |
| Relative Density. | 1.39 |
| Storage | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: Insoluble DMSO: 255 mg/mL (704.77 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (13.82 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||