货号	规格	价格	上海	北京	珠海	重庆	武汉
S81097-2mg买3赠1	99.90%	￥170.00 S81097-2mg ￥170.00 现货（买3赠1）	9 9	-	-	-	-
S81097-5mg买3赠1	99.90%	￥220.00 S81097-5mg ￥220.00 现货（买3赠1）	9 9	-	-	-	-
S81097-10mg买3赠1	99.90%	￥370.00 S81097-10mg ￥370.00 现货（买3赠1）	8 8	-	-	-	-
S81097-25mg买3赠1	99.90%	￥680.00 S81097-25mg ￥680.00 现货（买3赠1）	6 6	-	-	-	-
S81097-50mg促销	99.90%	￥1120.00 ￥896.00 S81097-50mg ￥896.00 现货	5 5	-	-	-	-
S81097-100mg促销	99.90%	￥1930.00 ￥1540.00 S81097-100mg ￥1540.00 现货	5 5	-	-	-	-
S81097-200mg促销	≥99%	￥2700.00 ￥2160.00 S81097-200mg ￥2160.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

IDO5L is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 67 nM.

靶点：

IDO:67 nM (IC50);IDO:19 nM (IC50, in HeLa cell)

体内研究：

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 (t1/2<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 (PBadjIC50=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 PBadjIC50 from 1.0 to 0.1 μM

参考文献：

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.

溶解性：

DMSO : ≥ 52 mg/mL (191.43 mM)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.681 ml	18.407 ml	36.813 ml
5 mM	0.736 ml	3.681 ml	7.363 ml
10 mM	0.368 ml	1.841 ml	3.681 ml
50 mM	0.074 ml	0.368 ml	0.736 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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INCB024360