| Identification | Back Directory | [Name]
IDO-IN-2 | [CAS]
1668565-74-9 | [Synonyms]
DO-IN-2
PCC0208009
IDO inhibitor 2
Urea, N-[4-[bis(2-methylpropyl)amino]-2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]-N'-(4-methylphenyl)-
PCC0208009,IDO,PCC-0208009,Inhibitor,Indoleamine 2,3-Dioxygenase (IDO),PCC 0208009,inhibit,neuropathic | [Molecular Formula]
C29H35N7O | [MOL File]
1668565-74-9.mol | [Molecular Weight]
497.63 |
| Chemical Properties | Back Directory | [density ]
1.206±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 10 mg/ml; DMSO: 10 mg/ml; Ethanol: 2 mg/ml; PBS (pH 7.2): insol | [form ]
A solid | [pka]
4.17±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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 [1][2]. | [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. |
| [IC 50]
IDO: 4.52 nM (IC50, in HeLa cell) | [References]
[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. DOI:10.1016/j.bcp.2020.113926
[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. DOI:10.1016/j.bmcl.2018.01.010
[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. DOI:10.1177/2058738418787991 |
|
|