产品
编 号:F199936
分子式:C29H35N7O
分子量:497.63
产品类型
结构图
CAS No: 1668565-74-9
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产品详情
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 .
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 brainare 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 brainwere observed at 60 min afteradministration.
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.
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 .