IDO5L is a potent inhibitor of IDO with an IC50 value of 19 nM in Hela cells[1].
体内研究
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].
体外研究
IDO5L is a potent inhibitor of IDO with an IC50 value of 19 nM in Hela cells[1].
作用机制
INCB024360 Analogue is a reversible and competitive inhibitor of IDO1, which can bound to IDO through the oxygen of the hydroxyamidine to the iron of the heme in the ferrous state.
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
Dose
Mice: min = 25 mg/kg, max = 100 mg/kg (s.c.) 25 mg/kg - 100 mg/kg (p.o.)
搜索
