IDO5L

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

IDO5L  纯度: 98.02%

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

IDO5L Chemical Structure

CAS No. : 914471-09-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550 In-stock
10 mg ¥500 In-stock
50 mg ¥1500 In-stock
100 mg ¥2500 In-stock
500 mg ¥6500 In-stock
1 g ¥10500 In-stock
5 g   询价  
10 g   询价  

* Please select Quantity before adding items.

IDO5L 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
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  • Anti-Cancer Compound Library
  • Small Molecule Immuno-Oncology Compound Library

生物活性

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

IC50 & Target[1]

IDO

67 nM (IC50)

IDO

19 nM (IC50, in HeLa cell)

体外研究
(In Vitro)

IDO5L (Compound 5l) is a potent (HeLa IC50=19 nM) inhibitor of IDO[1]. IDO5L is one of the highest potent inhibitors of the IDO1 (IC50=19 nM, in HeLa cell assay)[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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 (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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

271.64

Formula

C9H7ClFN5O2

CAS 号

914471-09-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 52 mg/mL (191.43 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6813 mL 18.4067 mL 36.8134 mL
5 mM 0.7363 mL 3.6813 mL 7.3627 mL
10 mM 0.3681 mL 1.8407 mL 3.6813 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.20 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.20 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.20 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.20 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.20 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.20 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

Animal Administration
[1]

Mice[1]
A single subcutaneous 100 mg/kg dose of IDO5L is administered to naive C57BL/6 mice bearing GM-CSF-secreting B16 tumors. Blood is harvested from individual mice over 8 h. Kynurenine and IDO5L concentrations are measured by LCMS. Reductions of kynurenine levels by 50-60% are observed between 2 and 4 h, with maximum inhibition seen at 2.5 h. Tumors are allowed to grow until day 7 when 14 days of subcutaneous dosing of IDO5L at 25, 50, and 75 mg/kg b.i.d. is initiated. Dose dependent inhibition of tumor growth is correlated with increasing exposures of IDO5L in plasma.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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