1. Metabolic Enzyme/Protease
  2. Indoleamine 2,3-Dioxygenase (IDO)
  3. PCC0208009

PCC0208009 

Cat. No.: HY-100771 Purity: 99.65%
Handling Instructions

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 .

For research use only. We do not sell to patients.

PCC0208009 Chemical Structure

PCC0208009 Chemical Structure

CAS No. : 1668565-74-9

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10 mM * 1 mL in DMSO USD 131 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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5 mg USD 120 In-stock
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10 mg USD 190 In-stock
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50 mg USD 590 In-stock
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Description

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].

IC50 & Target[1]

IDO

4.52 nM (IC50, in HeLa cell)

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[1].
PCC0208009 (0-200 nM; 48 hours) dose-dependently suppresses the IDO protein and mRNA expression induced by IFN-γ [3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

497.63

Formula

C29H35N7O

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (200.95 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (5.02 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.02 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: 99.65%

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PCC0208009
Cat. No.:
HY-100771
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