PCC0208009 是IDO有效的抑制剂，其在 HeLa 细胞中的IC50值为 4.52 nM。PCC0208009 通过调节 ACC 和杏仁核的突触可塑性来减轻神经性疼痛和合并症。
| 生物活性 | PCC0208009 is a potentIDOinhibitor with anIC50value of 4.52 nM in HeLa cell. PCC0208009 alleviates neuropathic pain and comorbidities by regulating synaptic plasticity of anterior cingulate cortex (ACC) and amygdala[1][2]. |
| IC50& Target[1] | IDO 4.52 nM (IC50, in HeLa cell) |
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体外研究
(In Vitro) | PCC0208009 inhibits IDO1 activity in HeLa cells, with anIC50value of 4.52 nM, but it does not change the enzyme activity in vitro, indicating that it acts as an indirect IDO1 inhibitor[1].
PCC0208009 (0-200 nM; 48 hours) dose-dependently suppresses the IDO protein and mRNA expression induced by IFN-γ[3].
Western Blot Analysis[3] | 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[3] | 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. |
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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[1].
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[1].
| Animal Model: | Adult male Sprague Dawley rats (180 g-200 g)[1] | | 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)[1] | | Dosage: | 12.5 mg/kg, 25 mg/kg, 50 mg/kg | | Administration: | oral gavage; once | | Result: | Showed the behavioral tests and the timelines. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(200.95 mM;Need ultrasonic) 配制储备液 | 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 |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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 (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。 2. 请依序添加每种溶剂： 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。 *以上所有助溶剂都可在本网站选购。
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