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IDO-IN-1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
IDO-IN-1图片
CAS NO:914638-30-5
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt316.1
Cas No.914638-30-5
FormulaC9H7BrFN5O2
Solubility≥29.1 mg/mL in DMSO; ≥25.9 mg/mL in EtOH; insoluble in H2O
Chemical Name4-amino-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
Canonical SMILESFC1=CC=C(/N=C(C2=NON=C2N)\NO)C=C1Br
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

IC50: 59 nM

IDO-IN-1 is an indoleamine-2,3-dioxygenase (IDO) inhibitor.

IDO is expressed in various tissues throughout the body but mainly in cells within the immune system where it is induced in dendritic cells and macrophages at sites of inflammation by cytokines. The overexpression of IDO has been implicated in a variety of diseases, such as cancer, neurodegenerative disorders, age-related cataract, and HIV encephalitis.

In vitro: In previous study, IDO-IN-1 was found to have improved in-vitro human intrinsic clearances without loss in IDO cellular potency [1].

In vivo: IDO-IN-1 analog, named 5l, was chosen for further in vivo studies because of its improved physical chemical properties compared to IDO-IN-1. The efficacy of 5l was tested in C57BL/6 mice with GMCSF-secreting B16 tumors, where 1-MT had previously shown activity. Results showed that the dose-dependent inhibition of tumor growth was linked to increasing exposures of 5l in plasma. In addition, a maximal effect of 50% tumor growth control (TGC) was observed when 5l was subcutaneously administered at 75 mg/kg bid. For comparison, 1-MT showed around 45% TGC when administered as subcutaneous pellets [1].

Clinical trial: Up to now, IDO-IN-1 is still in the preclinical development stage.

Reference:
[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.