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IDO5L

CAS No. : 914471-09-3

MCE 站：IDO5L

产品活性：IDO5L 是一种有效的吲哚胺-2,3-双加氧酶 (IDO) 抑制剂，IC₅₀ 为 67 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Indoleamine 2,3-Dioxygenase (IDO)

In Vitro: IDO5L (Compound 5l) is a potent (HeLa IC₅₀=19 nM) inhibitor of IDO. IDO5L is one of the highest potent inhibitors of the IDO1 (IC₅₀=19 nM, in HeLa cell assay).

In Vivo: Testing of IDO5L in mice demonstrates pharmacodynamic inhibition of IDO, as measured by decreased kynurenine levels (>50%) in plasma and dose dependent efficacy in mice bearing GM-CSF-secreting B16 melanoma tumors. Initial oral pharmacokinetic studies show that IDO5L is rapidly cleared (t_1/2<0.5 h) and that oral administration will not be a suitable dosing method for in vivo studies. The measured plasma exposure (2.5 μM) of IDO5L during this period exceeded our calculated mouse protein binding adjusted B16 cellular IC₅₀ (PB_adjIC₅₀=1.0 μM, murine cellular B16 IC₅₀=46 nM). Notably, kynurenine levels increase back to baseline after 4 h as IDO5L exposure levels decreased below the mouse PB_adjIC₅₀ from 1.0 to 0.1 μM.

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