产品
编 号：F741488
分子式：C27H29NO8
分子量：495.52
分子式：C27H29NO8
分子量：495.52
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 2293951-00-3
产品详情
生物活性：
Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue with anti-inflammatory activity. Anti-inflammatory agent 35 blocks mitogen-activated protein kinase (MAPK) signaling and p65 nuclear translocation of NF-kB. Anti-inflammatory agent 35 also inhibits yellow neutrophil infiltration and pro-inflammatory cytokine production. Anti-inflammatory agent 35 significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI) in vivo.
体内研究：
Anti-inflammatory agent 35 (化合物 5a27) (50 mg/kg；口服；单剂量，监测 0-25 分钟) 比姜黄素 (HY-N0005) 具有更好的生物利用度。Anti-inflammatory agent 35 (10 mg/kg；腹腔注射；每天 1 次，共 1 周) 通过抑制小鼠模型中的炎症改善 LPS 诱导的 ALI。在大鼠中的药代动力学参数RouteDose (mg/kg)AUC(0-t) (μg/L·h)AUC(0-∞) (μg/L·h)MRT(0-t) (h)MRT(0-∞) (h)t1/2 (h)Tmax (h)CLz/F (L/h/kg)Vz/F (L/kg)Cmax
p.o50231.2325.67.812.36.73.35062.6827.1113.3
i.v534.3122.411.319.90.20.1404.459.516.4
Animal Model:ALI mouse model (C57BL/6 mice)
Dosage:10 mg/kg
Administration:Intraperitoneal injection, once daily for 1 week; 30 min later every dose, followed by 5 mg/kg LPS, intratracheal injection
Result:Significantly normalized the wet/dry ratio of lungs.
体外研究：
Anti-inflammatory agent 35 (化合物 5a27) (10 μM；30 分钟) 抑制 LPS (0.5 μg/mL；24 小时) 对促炎细胞因子 (IL-6、TNF-α) 产生的诱导作用，对小鼠原代巨噬细胞没有细胞毒性。Anti-inflammatory agent 35 抑制 IL-6、TNF-α 的产生，IC50 分别为 2.23 μM 和 2.40 μM。Anti-inflammatory agent 35 (10 μM；30 分钟) 显着抑制 RAW 264.7 小鼠巨噬细胞中 LPS 诱导的激活。并且它显着抑制 p-p38 和 p-ERK，降低 IκB 水平，表明对 MAPK 和 NF-κB 信号的抑制。
Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue with anti-inflammatory activity. Anti-inflammatory agent 35 blocks mitogen-activated protein kinase (MAPK) signaling and p65 nuclear translocation of NF-kB. Anti-inflammatory agent 35 also inhibits yellow neutrophil infiltration and pro-inflammatory cytokine production. Anti-inflammatory agent 35 significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI) in vivo.
体内研究：
Anti-inflammatory agent 35 (化合物 5a27) (50 mg/kg；口服；单剂量，监测 0-25 分钟) 比姜黄素 (HY-N0005) 具有更好的生物利用度。Anti-inflammatory agent 35 (10 mg/kg；腹腔注射；每天 1 次，共 1 周) 通过抑制小鼠模型中的炎症改善 LPS 诱导的 ALI。在大鼠中的药代动力学参数RouteDose (mg/kg)AUC(0-t) (μg/L·h)AUC(0-∞) (μg/L·h)MRT(0-t) (h)MRT(0-∞) (h)t1/2 (h)Tmax (h)CLz/F (L/h/kg)Vz/F (L/kg)Cmax
p.o50231.2325.67.812.36.73.35062.6827.1113.3
i.v534.3122.411.319.90.20.1404.459.516.4
Animal Model:ALI mouse model (C57BL/6 mice)
Dosage:10 mg/kg
Administration:Intraperitoneal injection, once daily for 1 week; 30 min later every dose, followed by 5 mg/kg LPS, intratracheal injection
Result:Significantly normalized the wet/dry ratio of lungs.
体外研究：
Anti-inflammatory agent 35 (化合物 5a27) (10 μM；30 分钟) 抑制 LPS (0.5 μg/mL；24 小时) 对促炎细胞因子 (IL-6、TNF-α) 产生的诱导作用，对小鼠原代巨噬细胞没有细胞毒性。Anti-inflammatory agent 35 抑制 IL-6、TNF-α 的产生，IC50 分别为 2.23 μM 和 2.40 μM。Anti-inflammatory agent 35 (10 μM；30 分钟) 显着抑制 RAW 264.7 小鼠巨噬细胞中 LPS 诱导的激活。并且它显着抑制 p-p38 和 p-ERK，降低 IκB 水平，表明对 MAPK 和 NF-κB 信号的抑制。
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