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

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 .

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PCC0208009 Chemical Structure

PCC0208009 Chemical Structure

CAS No. : 1668565-74-9

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Based on 1 publication(s) in Google Scholar

PCC0208009 Related Antibodies

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View All Indoleamine 2,3-Dioxygenase (IDO) Isoform Specific Products:

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IDO1 IDO2 IDO

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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] .

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

PCC0208009 Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)CN(CC(C)C)C1=CC=C(C2=CC=CC=C2C3=NN=NN3)C=C1NC(NC4=CC=C(C)C=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (200.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.08%

COA (250 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0095 mL 10.0476 mL 20.0953 mL 50.2381 mL
5 mM 0.4019 mL 2.0095 mL 4.0191 mL 10.0476 mL
10 mM 0.2010 mL 1.0048 mL 2.0095 mL 5.0238 mL
15 mM 0.1340 mL 0.6698 mL 1.3397 mL 3.3492 mL
20 mM 0.1005 mL 0.5024 mL 1.0048 mL 2.5119 mL
25 mM 0.0804 mL 0.4019 mL 0.8038 mL 2.0095 mL
30 mM 0.0670 mL 0.3349 mL 0.6698 mL 1.6746 mL
40 mM 0.0502 mL 0.2512 mL 0.5024 mL 1.2560 mL
50 mM 0.0402 mL 0.2010 mL 0.4019 mL 1.0048 mL
60 mM 0.0335 mL 0.1675 mL 0.3349 mL 0.8373 mL
80 mM 0.0251 mL 0.1256 mL 0.2512 mL 0.6280 mL
100 mM 0.0201 mL 0.1005 mL 0.2010 mL 0.5024 mL
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PCC0208009 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PCC02080091668565-74-9PCC 0208009PCC-0208009Indoleamine 2,3-Dioxygenase (IDO)IDOneuropathicInhibitorinhibitorinhibit

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