Description | STING-IN-5, a potent inhibitor of the Stimulator of Interferon Genes (STING) pathway, significantly suppresses lipopolysaccharide (LPS)-induced nitric oxide (NO) synthesis in macrophages, exhibiting an IC50 of 1.15 μM. This compound dampens the inflammatory response and offers potential for research into anti-inflammatory diseases and sepsis [1]. |
In vitro | STING-IN-5(化合物30)(40 μM;24小时)对RAW264.7细胞的活力无显著影响[1]。在2.5 μM和5 μM浓度下,STING-IN-5(2小时处理)能显著抑制LPS诱导的RAW264.7细胞中的NO生成,其抑制率分别达到69.28 ± 2.36%和78.66 ± 2.73%,伴有IC50值为1.15 ± 0.15 μM[1]。此外,0.5-2 μM STING-IN-5(2小时处理)能够有效抑制STING以及下游的TBK1/IRF3/NF-κB信号通路的激活[1]。 |
In vivo | STING-IN-5(1.25-5 mg/kg;灌胃;每日一次,连续三天)在脓毒症小鼠中表现出对急性肝损伤的显著保护效果[1]。STING-IN-5在雄性Sprague-Dawley大鼠体内的药代动力学参数如下[1]:Tmax (h)、Cmax (ng/mL)、AUC 0-t (ng/mL·h)、AUC 0-∞ (ng/mL·h)、T 1/2 (h)、MRT 0-t (h) 以及 MRT 0-∞ (h) 分别为 1、66.52、81.08、135.7、1.11、0.99 和 2.02。 |
molecular weight | 854.17 |
Molecular formula | C47H67NO9S2 |
CAS | 2920064-17-9 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |