IDO5L is a potent inhibitor of IDO with an IC50 value of 19 nM in Hela cells[1].
IDO5L 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
HEK293 clone 6 cells
Function assay
Inhibition of human IDO1 transfected in HEK293 clone 6 cells by HPLC analysis
22616902
human HeLa cells
Function assay
Inhibition of indoleamine 2,3-dioxygenase in IFN-gamma-stimulated human HeLa cells assessed as kynurenine formation by spectrophotometry, IC50=19 nM
19507862
mouse B16 cells
Function assay
Inhibition of indoleamine 2,3-dioxygenase in mouse B16 cells assessed as kynurenine formation by spectrophotometry, IC50=46 nM
19507862
mouse P815B clone-6 cells
Function assay
Inhibition of human IDO1 transfected in mouse P815B clone-6 cells by HPLC analysis, IC50=60 nM
22616902
IDO5L 动物研究
Animal study
Evaluation of IDO5L in mice illustrates pharmacodynamic inhibition of IDO, as evidenced by decreased kynurenine levels (>50%) in plasma and dose-dependent efficacy in mice bearing GM-CSF-secreting B16 melanoma tumors. Initial oral pharmacokinetic studies reveal rapid clearance of IDO5L (t1/2<0.5 h), rendering oral administration unsuitable for in vivo studies. Plasma exposure measurements (2.5 μM) of IDO5L during this period surpass the calculated mouse protein binding-adjusted B16 cellular IC50 (PBadjIC50=1.0 μM, murine cellular B16 IC50=46 nM). Notably, kynurenine levels return to baseline after 4 hours as IDO5L exposure levels drop below the mouse PBadjIC50 from 1.0 to 0.1 μM[1].
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