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

IDO5L is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC 50 of 67 nM.

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IDO 67 nM (IC50) IDO 19 nM (IC50

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). has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC 50 (PB adj IC 50 =1.0 μM, murine cellular B16 IC 50 =46 nM). Notably, kynurenine levels increase back to baseline after 4 h as IDO5L exposure levels decreased below the mouse PB adj IC 50 from 1.0 to 0.1 μM. has not independently conf

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Powder -20°C 3 years；4°C 2 years

[1]. Yue EW, et al. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model. J Med Chem. 2009 Dec 10;52(23):7364-7.
[2]. Huang X, et al. Synthesis of [(18) F] 4-amino-N-(3-chloro-4-fluorophenyl)-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide (IDO5L): a novel potential PET probe for imaging of IDO1 expression. J Labelled Comp Radiopharm. 2015 Apr;58(4):156-62.

In Vitro: DMSO : ≥ 52 mg/mL (191.43 mM)配制储备液