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CAS No. : 1668565-74-9
MCE 国际站:PCC0208009
产品活性: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。
研究领域:Metabolic Enzyme/Protease
作用靶点:Indoleamine 2,3-Dioxygenase (IDO)
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 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.
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.
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