Resatorvid 是一种 Toll 样受体 4 的选择性抑制剂，可抑制NO、TNF-α和IL-6的产生。它下调TLR4下游信号分子 MyD88 和 TRIF 的表达。它抑制自噬，有抗炎作用。

Resatorvid (TAK-242) is a selective inhibitor of Toll-like receptor 4 (TLR4). Resatorvid inhibits IL-6, TNF-R and NO production (IC50s: 1.3 nM, 1.9 nM, and 1.8 nM).

Resatorvid suppresses the production of NO, TNF-α, and IL-6 from LPS-stimulated human peripheral blood mononuclear cells (PBMCs, IC50s: 11-33 nM). Resatorvid (1-100 nM; 15 minutes; PBMCs cells) markedly inhibits the LPS-induced phosphorylation of extracellular signal-regulated kinase 1/2 (Erk1/2), p38, and JNK/SAPK as well as degradation of IκBβ at a concentration of 100 nM. Resatorvid (1-100 nM; 4 hours) inhibits mRNA expression of IL-6 and TNF-α induced by LPS and IFN-γ in RAW264.7 cells [1].

In ApoE knockout and wild-type mice, Resatorvid (0.3?mg/kg; intraperitoneal injection; twice a week; for 4 weeks) treatment inhibits serum autoantibodies (ANA and anti-dsDNA), cytokines (IFN-γ, TNF-α, IL-1β), lung inflammation, and intima-media thickness in brachiocephalic artery [2].

Cell Line: RAW264.7 cells. Concentration: 1 nM, 10 nM, 100 nM. Incubation Time: 4 hours [1]

Animal Model: 30 ApoE knockout and 30 wild-type mice on a C57BL/6 background (female, 10 weeks old). Dosage: 0.3?mg/kg. Administration: i.p.; twice a week; for 4 weeks [3]

243984-11-4

C15H17ClFNO4S

361.82

瑞沙托维;CLI-095;TAK-242

H2O:Insoluble
DMSO:100 mg/mL (276.38 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years