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TAK-242 (Resatorvid)

Cat. No. M4838
TAK-242 (Resatorvid) Structure
Synonym:

Resatorvid; CLI-095

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 70  USD70 In stock
5mg USD 114  USD114 In stock
10mg USD 178  USD178 In stock
25mg USD 378  USD378 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
Source Mar Drugs (2020), Figure 9, TAK-242 (Abmole Bioscience)
Method pre-incubated cells
Cell Lines RAW264.7 cells
Concentrations 10 µmol/L
Incubation Time 1h
Results This result suggested that TLR4 was one of the receptors of PSP-L on RAW264.7 cells and may be the vital one.
Source Mar Drugs (2020), Figure 8, TAK-242 (Abmole Bioscience)
Method pre-incubated cells
Cell Lines RAW264.7 cells
Concentrations 10 µmol/L
Incubation Time 1h
Results This result suggested that TLR4 was one of the receptors of PSP-L on RAW264.7 cells and may be the vital one.
Source Oncotarget (2018). Figure 3. TAK-242
Method Western blotting
Cell Lines RA-FLS cells
Concentrations -
Incubation Time 24, 48 and 72 h.
Results As shown in Figure 3, the protein and mRNA expressions of TLR4 and NF-κB decreased in the miR-146a mimic and the Tak-242 groups, while mRNA and protein expressions of TLR4 and NF- κB increased in the miR-146a inhibitor and the TLR4 groups, and the mRNA and protein expressions of TLR4 and NF-κB in the TLR4 group were significantly higher than those in the miR-146a inhibitor group
Protocol (for reference only)
Cell Experiment
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
Animal models C57Bl/6 mice
Formulation 5% DMSO, 5% Tween80
Dosages 3 mg/kg
Administration i.v.
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Fei Xing, et al. Mol Pain. TLR4/NF-κB signaling activation in plantar tissue and dorsal root ganglion involves in the development of postoperative pain

[2] Woller SA, et al. Brain Behav Immun. Systemic TAK-242 prevents intrathecal LPS evoked hyperalgesia in male, but not female mice and prevents delayed allodynia following intraplantar formalin in both male and female mice: The role of TLR4 in the evolution of a persistent pain state

[3] Hussey SE, et al. Biosci Rep. TAK-242, a small-molecule inhibitor of Toll-like receptor 4 signalling, unveils similarities and differences in lipopolysaccharide- and lipid-induced inflammation and insulin resistance in muscle cells.

[4] Takuryu Sha, et al. Shock. Combination of imipenem and TAK-242, a Toll-like receptor 4 signal transduction inhibitor, improves survival in a murine model of polymicrobial sepsis

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  Catalog
Abmole Inhibitor Catalog




Keywords: TAK-242 (Resatorvid), Resatorvid; CLI-095 supplier, TLR, inhibitors, activators


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