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编 号：F753464
分子式：C28H23N3O4S
分子量：497.56
分子式：C28H23N3O4S
分子量：497.56
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CAS No: 2506823-08-9
产品详情
生物活性：
BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury.
体内研究：
BET-IN-13 (3 mg/kg；静脉注射；一次) 在小鼠中显示出良好的药代动力学 (PK) 特性，T1/2 为 0.69 h，AUCINF-obs 为 609 h*ng/mL 和 Vss 为 1717 mL/kg。BET-IN-13 (37.5、75 mg/kg；腹腔注射；一次) 降低 LPS/D-GalN(d-gaiactosamine)诱导的急性肝衰竭 (ALF) 小鼠的炎症和肝损伤而无明显毒性。Animal Model:20-22g, Female C57BL/6J mice (LPS/D-GalN(d-gaiactosamine)-induced acute liver failure (ALF))
Dosage:37.5, 75 mg/kg
Administration:I.p.; once
Result:Reduced inflammatory responses associated with LPS/GalN-induced acute liver failure with the survival rate increased significantly to 69.2% for37.5 mg/kg and to 84.6% for 75 mg/kg.
体外研究：
BET-IN-13 (compound 28) (1.1, 3.3, 10 μM, 2+6 h) 降低 RAW264.7 细胞中 LPS (500 ng/ml) 诱导的 TNF-α、IL-1β、IL-6 和 NOS2 mRNA 的表达水平。
BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury.
体内研究：
BET-IN-13 (3 mg/kg；静脉注射；一次) 在小鼠中显示出良好的药代动力学 (PK) 特性，T1/2 为 0.69 h，AUCINF-obs 为 609 h*ng/mL 和 Vss 为 1717 mL/kg。BET-IN-13 (37.5、75 mg/kg；腹腔注射；一次) 降低 LPS/D-GalN(d-gaiactosamine)诱导的急性肝衰竭 (ALF) 小鼠的炎症和肝损伤而无明显毒性。Animal Model:20-22g, Female C57BL/6J mice (LPS/D-GalN(d-gaiactosamine)-induced acute liver failure (ALF))
Dosage:37.5, 75 mg/kg
Administration:I.p.; once
Result:Reduced inflammatory responses associated with LPS/GalN-induced acute liver failure with the survival rate increased significantly to 69.2% for37.5 mg/kg and to 84.6% for 75 mg/kg.
体外研究：
BET-IN-13 (compound 28) (1.1, 3.3, 10 μM, 2+6 h) 降低 RAW264.7 细胞中 LPS (500 ng/ml) 诱导的 TNF-α、IL-1β、IL-6 和 NOS2 mRNA 的表达水平。
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