TAK-242 (Resatorvid), a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4. IC50 value: 1.1-11 nM Target: TLR4 in vitro: In RAW264.7 cells and mouse peritoneal macrophages, TAK-242 suppressed lipopolysaccharide (LPS)-induced production of NO, tumor necrosis factor-alpha (TNF-alpha), and interleukin (IL)-6, with 50% inhibitory concentration (IC50) of 1.1 to 11 nM. TAK-242 also suppressed the production of these cytokines from LPS-stimulated human peripheral blood mononuclear cells (PBMCs) at IC50 values from 11 to 33 nM. In addition, the inhibitory effects on the LPS-induced IL-6 and IL-12 production were similar in human PBMCs, monocytes, and macrophages. TAK-242 inhibited mRNA expression of IL-6 and TNF-alpha induced by LPS and interferon-gamma in RAW264.7 cells . TAK-242 selectively bound to TLR4. The time course of the inhibitory effect of TAK-242 on inflammatory mediator production corresponded to that of the binding of TAK-242 to TLR4. TAK-242 inhibited the association of TLR4 with Toll/interleukin-1 receptor domain-containing adaptor protein (TIRAP) or Toll/interleukin-1 receptor domain-containing adaptor protein inducing interferon-β-related adaptor molecule (TRAM) in human embryonic kidney (HEK) 293 cells overexpressing TLR4, MD-2, and TIRAP or TRAM, respectively . in vivo: To evaluate the effect of blocking TLR4 on visceral nociception, TAK-242, a selective TLR4 antagonist, was administered peripherally (intravenous) and centrally (intracerebroventricular and intra-PFC) (n = 10-12/experimental group) . Intravenous administration of TAK-242 to mice 1 h be Fore LPS challenge dose-dependently inhibited LPS-induced increases in serum levels of TNF-alpha, IL-1beta, IL-6, IL-10, MIP-2, and NO metabolites. TAK-242 protected mice from LPS-induced lethality in a similar dose-dependent manner, and rescued 100% of mice at a dose of 1 mg/kg. Interestingly, TAK-242 worked quickly, and showed beneficial effects even when administered after LPS challenge .For the detailed information of TAK-242 (Resatorvid), the solubility of TAK-242 (Resatorvid) in water, the solubility of TAK-242 (Resatorvid) in DMSO, the solubility of TAK-242 (Resatorvid) in PBS buffer, the animal experiment (test) of TAK-242 (Resatorvid), the cell expriment (test) of TAK-242 (Resatorvid), the in vivo, in vitro and clinical trial test of TAK-242 (Resatorvid), the EC50, IC50,and Affinity of TAK-242 (Resatorvid), Please contact DC Chemicals.
| CAS No. | 243984-11-4 |
| Chemical Name | TAK-242 (Resatorvid) |
| Synonyms | Resatorvid; TAK242; TAK 242 |
| SMILES | CCOC(=O)C1=CCCC[C@H]1S(=O)(=O)NC2=C(C=C(C=C2)F)Cl |
| Formula | C15H17ClFNO4S |
| M.Wt | 361.82 |
| Purity | >98% |
| Storage | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Shipping condition | Ships from Shanghai; packaging confirmed at order. |
| Publication | Not available |
| Product classification | Adjuvant Molecules |
The product molecular weight is prefilled when available and remains editable. Confirm solvent compatibility and solubility before preparation.
Solvent volumes update from the molecular weight above.
| Mass | 1 mM | 5 mM | 10 mM |
|---|---|---|---|
| 10 mg | 27.6381 mL | 5.5276 mL | 2.7638 mL |
| 25 mg | 69.0951 mL | 13.8190 mL | 6.9095 mL |
| 50 mg | 138.1903 mL | 27.6381 mL | 13.8190 mL |
| 100 mg | 276.3805 mL | 55.2761 mL | 27.6381 mL |
| 250 mg | 690.9513 mL | 138.1903 mL | 69.0951 mL |
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