TAK-242

TLR4

361.82

DMSO : 100 mg/mL (276.38 mM)
Ethanol : 20 mg/mL (55.28 mM)

Off-white to yellow Solid

In RAW264.7 cells and mouse peritoneal macrophages, Resatorvid (TAK-242) suppresses lipopolysaccharide (LPS)-induced production of NO, tumor necrosis factor-α (TNF-α), and interleukin (IL)-6, with IC50 of 1.1 to 11 nM. Resatorvid (TAK-242) also suppresses the production of these cytokines from LPS-stimulated human peripheral blood mononuclear cells (PBMCs) at IC50 values from 11 to 33 nM.

Resatorvid (TAK-242) apparently reduces the serum anti-dsDNA levels in both genotype mice. Alternatively, IFN-γ, TNF-α, and IL-1β production is markedly inhibited by Resatorvid (TAK-242), but their concentrations are still greatly higher than those in NS-treated counterparts. Resatorvid (TAK-242) pre-stress administration prevents the accumulation of potentially deleterious inflammatory and oxidative/nitrosative mediators in the brain frontal cortex of rats. Resatorvid (TAK-242) i.v. administration at the beginning of the stress session completely blocks TLR-4 mRNA and protein upregulation after stress exposure.

瑞沙托维

C₁₅H₁₇ClFNO₄S

243984-11-4