Resatorvid (TAK-242) is a selective TLR4 signaling inhibitor. Resatorvid inhibited the production of NO, TNF-α and IL-6 with IC50 values of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid down-regulates the expression of MyD88 and TRIF signaling molecules downstream of TLR4. Resatorvid inhibits autophagy and plays a key role in a variety of inflammatory diseases.
Chem Biodivers. 2023 Jan 18.
Cinnamaldehyde ameliorates dextran sulfate sodium‐induced colitis in mice by modulating TLR4/NF‐κB signaling pathway and NLRP3 inflammasome activation
TAK-242 (Resatorvid) purchased from AbMole
Thromb Res. 2023 Feb;222:49-62.
High mobility group box 1 derived mainly from platelet microparticles exacerbates microvascular obstruction in no reflow
TAK-242 (Resatorvid) purchased from AbMole
Front Immunol. 2022 Jul 8;13:901566.
Hepatocyte-Conditional Knockout of Phosphatidylethanolamine Binding Protein 4 Aggravated LPS/D-GalN-Induced Acute Liver Injury via the TLR4/NF-κB Pathway
TAK-242 (Resatorvid) purchased from AbMole
Animals (Basel). 2021 Dec 1;11(12):3422..
NF-κB–Dependent Snail Expression Promotes Epithelial–Mesenchymal Transition in Mastitis
TAK-242 (Resatorvid) purchased from AbMole
Clinics (Sao Paulo). 2021 Mar 8;76:e2484.
miR-139-5p protects septic mice with acute lung injury by inhibiting Toll-like receptor 4/Myeloid differentiation factor 88/Nuclear factor-&mac_kgr;B signaling pathway
TAK-242 (Resatorvid) purchased from AbMole
Mar Drυgs. 2020 Oct 28;18(11):538.
Immunostimulatory Effects of Polysaccharides from Spirulina platensis In Vivo and Vitro and Their Activation Mechanism on RAW246.7 Macrophages
TAK-242 (Resatorvid) purchased from AbMole
Mar Drυgs. 2020 Aug 17;18(8):429.
Comparison of Physicochemical Characteristics and Macrophage Immunostimulatory Activities of Polysaccharides from Chlamys farreri
TAK-242 (Resatorvid) purchased from AbMole
Biochem Biophys Res Commun. 2020 Oct 22;531(4):602-608.
Toll-like receptor 4 plays a key role in advanced glycation end products-induced M1 macrophage polarization
TAK-242 (Resatorvid) purchased from AbMole
J Clin Invest. 2020 May 19.
Residual endotoxin induces primary graft dysfunction through ischemia-reperfusion-primed alveolar macrophages
TAK-242 (Resatorvid) purchased from AbMole
Cell Mol Neurobiol. 2019 Mar;39(2):301-319.
Myosin IIA Regulated Tight Junction in Oxygen Glucose-Deprived Brain Endothelial Cells Via Activation of TLR4/PI3K/Akt/JNK1/2/14-3-3ε/NF-κB/MMP9 Signal Transduction Pathway.
TAK-242 (Resatorvid) purchased from AbMole
Cell Experiment | |
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Cell lines | L6-GLUT4myc |
Preparation method | Prior to treatment with LPS or stearate, cells were pre-treated with TAK-242 (1 μM) or vehicle control for 1 h. TAK-242 remained in culture medium for the duration for the experiment. |
Concentrations | 1 μM |
Incubation time | 1 h |
Animal Experiment | |
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Animal models | C57Bl/6 mice |
Formulation | 5% DMSO, 5% Tween80 |
Dosages | 3 mg/kg |
Administration | i.v. |
Molecular Weight | 361.82 |
Formula | C15H17ClFNO4S |
CAS Number | 243984-11-4 |
Solubility (25°C) | DMSO 80 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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