Free shipping on all orders over $ 500

TAK-242 (Resatorvid)

Cat. No. M4838

All AbMole products are for research use only, cannot be used for human consumption.

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
Free Delivery on orders over USD 500 Bulk Inquiry?

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
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

Related TLR Products
Pepinh-TRIF TFA

Pepinh-TRIF TFA blocks TIR-domain-containing adapter-inducing interferon-β (TRIF) signaling by interfering with TLR-TRIF interaction.

CAY10614

CAY10614 is a potent TLR4 antagonist. CAY10614 inhibits the lipid A-induced activation of TLR4, with an IC50 of 1.675 μM.

TLR4-IN-C34-C2-COOH

TLR4-IN-C34-C2-COO is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

BNT411 

BNT411 is a selective TLR7 agonist that can induce the release of IFNa both in vivo and in vitro.

Rabeximod

Rabeximod (ROB-803), an anti-rheumatic compound, impairs the differentiation and function of human pro-inflammatory dendritic cells and macrophages via downregulating TLR2 and TLR4 stimulation.

  Catalog
Abmole Inhibitor Catalog




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

All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.



Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.