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IDO5L

CAS No. : 914471-09-3

MCE 国际站：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.

相关产品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Small Molecule Immuno-Oncology Compound Library  |  Human Metabolite Library  |  Metabolic Enzyme Compound Library  |  Multi-Target Compound Library  |  Bioactive Compound Library Max  |  Necrostatin-1  |  3-TYP  |  Epacadostat  |  Indoximod  |  Linrodostat  |  β-Lapachone  |  Palmatine chloride  |  Navoximod  |  Coptisine chloride  |  IDO-IN-7  |  PF-06840003  |  DP00477  |  IACS-8968  |  GNF-PF-3777  |  LY-3381916  |  IDO1/TDO-IN-4  |  IDO2-IN-1  |  PCC0208009  |  IDO-IN-3  |  PROTAC IDO1 Degrader-1  |  Coptisine Sulfate  |  BMS-978587  |  BMT-297376  |  IDO-IN-1  |  IDO-IN-18

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