IDO-IN-2|1668565-74-9|-陌孚医药/Medlife

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IDO-IN-2

目录号: PC16970 纯度: ≥98%

CAS No. :1668565-74-9

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中文名称

IDO-IN-2

中文别名

IDO-IN-2

英文名称

IDO-IN-2

英文别名

IDO-IN-2;IDO-IN2;1-[2-[bis(2-methylpropyl)amino]-5-[2-(2H-tetrazol-5-yl)phenyl]phenyl]-3-(4-methylphenyl)urea;Urea, N-[4-[bis(2-methylpropyl)amino]-2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]-N'-(4-methylphenyl)-;AMY16308;BCP20804;BDBM50454785;AK685633;S8557;1-(4-(Diisobutylamino)-2'-(1H-tetrazol-5-yl)biphenyl-3-yl)-3-p-tolylurea;PCC0208009;DO-IN-2;C73217

Cas No.

1668565-74-9

分子式

C₂₉H₃₅N₇O

分子量

497.63

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

PCC0208009 is a potent IDO inhibitor with an IC₅₀ value of 4.52 nM in HeLa cell. PCC0208009 alleviates neuropathic pain and comorbidities by regulating synaptic plasticity of anterior cingulate cortex (ACC) and amygdala .

性状

Solid

IC50 & Target[1][2]

IDO

4.52 nM (IC₅₀, in HeLa cell)

体外研究(In Vitro)

PCC0208009 inhibits IDO1 activity in HeLa cells, with an IC₅₀ value of 4.52 nM, but it does not change the enzyme activity 体外研究, indicating that it acts as an indirect IDO1 inhibitor.
PCC0208009 (0-200 nM; 48 hours) dose-dependently suppresses the IDO protein and mRNA expression induced by IFN-γ.

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

Western Blot Analysis

Cell Line:	HeLa cells
Concentration:	0, 50, 100, 200 nM
Incubation Time:	48 hours
Result:	The IDO protein expression induced by IFN-γ was dose-dependently suppressed by PCC, which showed significant differences at 100 and 200?nM (P?<?0.05).

RT-PCR

Cell Line:	HeLa cells
Concentration:	0, 50, 100, 200 nM
Incubation Time:	48 hours
Result:	The IDO mRNA expression induced by IFN-γ was dose-dependently suppressed by PCC, which showed significant differences at all doses compared with the IFN-γ group.

体内研究(In Vivo)

PCC0208009 (single oral gavage; 50 mg/kg) in adult male Sprague Dawley rats (180 g-200 g) is detected at 60, 120 and 240 min after drug administration in plasma and brain samples, and the highest concentrations of PCC0208009 in plasma and brain are observed at 60 min after administration. Concomitantly, the Kyn/Trp ratio decreases at 60, 120 and 240 min postdose, with the minimum level in the plasma and the brain seen at 60 min post-dose.
PCC0208009 (oral gavage; once; 12-50 mg/kg) in adult male Sprague Dawley rats (180 g-200 g) is detected at 30, 60 and 90min after administration to evaluate the antinociceptive effects of PCC0208009 on neuropathic pain.

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

Animal Model:	Adult male Sprague Dawley rats (180 g-200 g)
Dosage:	50 mg/kg
Administration:	Single oral gavage
Result:	The highest concentrations of PCC0208009 in plasma and brain were observed at 60 min after administration.

Animal Model:	Adult male Sprague-Dawley rats bearing spinal nerve ligation (SNL)
Dosage:	12.5 mg/kg, 25 mg/kg, 50 mg/kg
Administration:	oral gavage; once
Result:	Showed the behavioral tests and the timelines.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Yu Wang, et al. PCC0208009, an indirect IDO1 inhibitor, alleviates neuropathic pain and co-morbidities by regulating synaptic plasticity of ACC and amygdala. Biochem Pharmacol. 2020 Jul;177:113926. [Information]

[2]. David K Williams, et al. Development of a series of novel o-phenylenediamine-based indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. Bioorg Med Chem Lett. 2018 Feb 15;28(4):732-736. [Information]

[3]. Shanyue Sun, et al. PCC0208009 enhances the anti-tumor effects of temozolomide through direct inhibition and transcriptional regulation of indoleamine 2,3-dioxygenase in glioma models. Int J Immunopathol Pharmacol. Jan-Dec 2018;32:2058738418787991. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (200.95 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0095 mL	10.0476 mL	20.0953 mL
5 mM	0.4019 mL	2.0095 mL	4.0191 mL
10 mM	0.2010 mL	1.0048 mL	2.0095 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (5.02 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.02 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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 ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.02 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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