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编 号:F750581
分子式:C32H46N2O3
分子量:506.72
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1mg
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5mg
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生物活性:
STING-IN-4 (Compound 1) is a STING inhibitor that inhibits STING expression and hence reducing activation of STING and nuclear factor-κB (NF-κB) signaling. STING-IN-4 shows anti-inflammatory activity and can be used for the research of sepsis.

体内研究:
STING-IN-4 (Compound 1) (1-9 mg/kg; i.p.; daily for 3 days) 保护 LPS 诱导的小鼠肝损伤,抑制脓毒症小鼠肝脏 STING/IRF3/NF-κB 激活。Animal Model:BALB/c mice, LPS-induced acute liver injury model
Dosage:1, 3 and 9 mg/kg
Administration:Intraperitoneal injection, daily for 3 days
Result:Significantly reduced the hemorrhage severity. Decreased the levels of alanine transaminase (ALT), aspartate aminotransferase (AST), and alkaline phosphatase (ALP) induced by LPS. Significantly reduced the levels of TNF-α, IL-6, and IFN-β compared with mice treated only with LPS. Markedly reduced the levels of STING, p-TBK, p-IRF3, p-p65, and p-IκB-α.

体外研究:
STING-IN-4 (Compound 1) (20 μM; 26 h) 抑制 LPS 诱导 RAW264.7 细胞产生 NO。STING-IN-4 (2.5-10 μM; 26 h) 显著抑制 RAW264.7 细胞中 iNOS 的表达。STING-IN-4 (5 and 50 μM; 12 h) 在 49、52 和 55 °C时显著降低 STING 的降解,并可能与 STING 相互作用并增强 STING 的热稳定性。STING-IN-4 (2.5-10 μM; 8 h) 抑制 LPS 诱导的 STING/IRF3/NF-κB 的激活。
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