BET-IN-13 是一种有效的BET抑制剂，IC50值为 1.6 nM。BET-IN-13 降低 LPS 诱导的 TNF-α、IL-1β、IL-6 和 NOS2 mRNA 表达水平。BET-IN-13 具有抗炎活性。BET-IN-13 具有研究急性肝损伤的潜力。
| 生物活性 | BET-IN-13 is a potentBETinhibitor with anIC50value 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[1]. |
| IC50& Target[1] | BRD4 BD1 57.4 nM (IC50) | BRD4 BD2 44.4 nM (IC50) | BRD2 BD1 79.3 nM (IC50) | BRD2 BD2 27.5 nM (IC50) | BRD3 BD1 45.6 nM (IC50) | BRD3 BD2 18.9 nM (IC50) | BRDT BD1 87.0 nM (IC50) | BRDT BD2 43.4 nM (IC50) |
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体外研究
(In Vitro) | 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[1]。
RT-PCR[1] | Cell Line: | RAW264.7 cells | | Concentration: | 1.1, 3.3, 10 μM | | Incubation Time: | Pre-treated for 2 h before stimulating with LPS for 6 h | | Result: | Significantly reduced LPS (500 ng/ml) induced TNF-α, IL-1β, IL-6 and NOS2 mRNA expression levels in a dose-dependent manner. |
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体内研究
(In Vivo) | 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[1]。
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[1]。
| Animal Model: | 20-22g, Female C57BL/6J mice (LPS/D-GalN(d-gaiactosamine)-induced acute liver failure (ALF))[1] | | 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. |
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| 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. |
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