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STING-IN-5 is a potent STING inhibitor, inhibiting LPS-induced NO synthesis in macrophages with an IC50 value 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]. | [in vivo]
STING-IN-5 (1.25-5 mg/kg; i.g.; once daily; for 3 days) have an obvious protective effect on acute liver injury in septic mice[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).
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| [References]
[1] Long J, et al. Discovery of fusidic acid derivatives as novel STING inhibitors for treatment of sepsis. Eur J Med Chem. 2022 Dec 15;244:114814. DOI:10.1016/j.ejmech.2022.114814 |
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