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编 号:F751304
分子式:C25H22F4N2O3
分子量:474.45
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
IDO1-IN-19 (Compound 17) is an orally active IDO1 inhibitor with an IC50 of CYP2C9 of 8.64 μM. IDO1-IN-19 also acts funciton on cardiac channels, with IC50s of 12 μM (IKr), 40 μM (INa), 8.3 μM (ICa), respectively. IDO1-IN-19 has the potential to study cancer diseases.

体内研究:
IDO1-IN-19 (0.3-30 mg/kg; 口服; 单剂量) 可降低 hIDO1 转基因荷瘤小鼠的肿瘤中的 Kyn 水平 (Kyn 是 IDO 在体内催化 Trp 的代谢产物)。IDO1-IN-19 的药代动力学分析AnimalRouteDose (mg/kg)Cl (mL/min/kg)t1/2 (h)F (%) (SDD)F (%) crystallinefu'p
Rat (Wistar Han)IV/PO0.5/1.010.67.462277.7
DogIV/PO0.25/0.51.04350163.3
Animal Model:CT26 tumor-bearing model in hIDO1-konck-in mice
Dosage:0.3 mg/kg, 3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration:po, single dose; euthanized mouse at 2, 4, 8, 16, and 24 h following dose.
Result:Resulted dose-dependent reduction of Kyn both in plasma and tumor.
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