STING-IN-5 是一种有效的STING抑制剂，在巨噬细胞中抑制 LSP 诱导的 NO 合成，IC50为 1.15 μM。STING-IN-5 抑制炎症反应。STING-IN-5 可用于研究抗炎疾病和败血症。
| 生物活性 | STING-IN-5 is a potentSTINGinhibitor, inhibiting LPS-inducedNO synthesisin macrophages with anIC50value of 1.15 μM. STING-IN-5 inhibits the inflammatory response. STING-IN-5 can be used to research anti-inflammatory diseases and sepsis[1]. |
体外研究
(In Vitro) | STING-IN-5 (化合物30) (40 μM; 24 h) 对 RAW264.7 细胞活力影响较小[1]。
STING-IN-5 (2.5 和 5 μM; 2 h) 抑制 LPS 刺激的 RAW264.7 细胞产生 NO，在 2.5 μM 和 5 μM 下的抑制率分别为 69.28 ± 2.36% 和 78.66 ± 2.73%，IC50为 1.15 ± 0.15 μM[1]。
STING-IN-5 (0.5-2 μM; 2 h) 抑制 STING，以及 TBK1/IRF3/NF-κB 激活[1]。
Cell Viability Assay[1] | Cell Line: | RAW264.7 | | Concentration: | 40 μM | | Incubation Time: | 24 h | | Result: | Exhibited less effect on RAW264.7 cell viability of 91.08 ± 1.09% |
Western Blot Analysis[1] | Cell Line: | RAW264.7 (stimulated by LPS for 6 h) | | Concentration: | 0.5, 1 and 2 μM | | Incubation Time: | 2 h | | Result: | Significantly inhibited the protein expression of STING and the phosphorylation of the downstream targets TBK1, IRF3, p65, and IκB in a concentration-dependent manner. |
|
体内研究
(In Vivo) | STING-IN-5 (1.25-5 mg/kg；灌胃；每日 1 次，连续 3 天) 对脓毒症小鼠急性肝损伤有明显保护作用[1]。
Pharmacokinetic Parameters of STING-IN-5 in male Sprague-Dawley rats[1].
| Tmax(h) | Cmax(ng/mL) | AUC0-t(ng/mL·h) | AUC0-∞(ng/mL·h) | T1/2(h) | MRT0-t(h) | MRT0-∞(h) | | 1 | 66.52 | 81.08 | 135.7 | 1.11 | 0.99 | 2.02 |
| Animal Model: | Male BALB/c mice (6-8 weeks; acute liver injury induced by injection of 10 mg/kg LPS)[1] | | Dosage: | 1.25, 2.5, 5 mg/kg | | Administration: | i.g.; once daily; for 3 days | | Result: | Significantly improved pathological changes including disorderly arranged liver cells, blurred boundaries, congested hepatic sinusoids, swollen hepatocytes, a small number of hepatocytes were necrotic, and inflammatory cells infiltrated local areas.
Significantly reduced the levels of AST, ALT, and ALP (liver function specific indicators). |
|
| 分子量 | |
| Formula | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com