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• 产品描述： 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

• 靶点： IDO:4.52 nM (IC50, in HeLa cell);Indoleamine2,3-Dioxygenase(IDO)

• 体外研究：
  PCC0208009 inhibits IDO1 activity in HeLa cells, with an IC50 value of 4.52 nM, but it does not change the enzyme activity in vitro, 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. 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：
  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. 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.

• 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.
  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.
  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.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.01 ml	10.048 ml	20.095 ml
  5 mM	0.402 ml	2.01 ml	4.019 ml
  10 mM	0.201 ml	1.005 ml	2.01 ml
  50 mM	0.04 ml	0.201 ml	0.402 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *