产品
编 号：F756863
分子式：C47H67NO9S2
分子量：854.17
分子式：C47H67NO9S2
分子量：854.17
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2920064-17-9
产品详情
生物活性：
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.
体内研究：
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。Pharmacokinetic Parameters of STING-IN-5 in male Sprague-Dawley rats.Tmax (h)Cmax (ng/mL) AUC0-t (ng/mL·h)AUC0-∞ (ng/mL·h)T1/2 (h)MRT0-t (h)MRT0-∞ (h)
166.5281.08135.71.110.992.02
Animal Model:Male BALB/c mice (6-8 weeks; acute liver injury induced by injection of 10 mg/kg LPS)
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).
体外研究：
STING-IN-5 (化合物30) (40 μM; 24 h) 对 RAW264.7 细胞活力影响较小。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。STING-IN-5 (0.5-2 μM; 2 h) 抑制 STING，以及 TBK1/IRF3/NF-κB 激活。
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.
体内研究：
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。Pharmacokinetic Parameters of STING-IN-5 in male Sprague-Dawley rats.Tmax (h)Cmax (ng/mL) AUC0-t (ng/mL·h)AUC0-∞ (ng/mL·h)T1/2 (h)MRT0-t (h)MRT0-∞ (h)
166.5281.08135.71.110.992.02
Animal Model:Male BALB/c mice (6-8 weeks; acute liver injury induced by injection of 10 mg/kg LPS)
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).
体外研究：
STING-IN-5 (化合物30) (40 μM; 24 h) 对 RAW264.7 细胞活力影响较小。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。STING-IN-5 (0.5-2 μM; 2 h) 抑制 STING，以及 TBK1/IRF3/NF-κB 激活。
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