TAK-242

TLR4拮抗剂（在SEAP测定中IC50=0.68µM）；100nM时选择性结合TLR4而非TLR1-3和TLR5-10；1µM时阻止TLR4与表达人类受体的HEK293细胞中的TIRAP或TRAM相互作用；抑制分离的小鼠腹膜巨噬细胞中IFN-γ和LPS诱导的NO、TNF-α、IL-6和IL-1β的产生（IC50s=5.7-11nM）；5-20µM时抑制分离的人类中性粒细胞中LPS诱导的NETosis；0.3、1和3mg/kg时提高LPS诱导的脓毒症休克小鼠模型的存活率。A TLR4 antagonist (IC50 = 0.68 µM in a SEAP assay); selectively binds to TLR4 over TLR1-3 and TLR5-10 at 100 nM; prevents the interaction of TLR4 with TIRAP or TRAM in HEK293 cells expressing the human receptors at 1 µM; inhibits IFN-γ- and LPS-induced production of NO, TNF-α, IL-6, and IL-1β in isolated mouse peritoneal macrophages (IC50s = 5.7-11 nM); inhibits LPS-induced NETosis in isolated human neutrophils at 5-20 µM; improves survival in a mouse model of LPS-induced septic shock at 0.3, 1, and 3 mg/kg.