2. Metabolic Enzyme/Protease
  3. Indoleamine 2,3-Dioxygenase (IDO)
  4. IDO1/TDO-IN-4

IDO1/TDO-IN-4 is a potent IDO1/TDO dual inhibitor, with IC50 values of 3.53 μM (IDO1) and 1.15 μM (TDO). IDO1/TDO-IN-4 forms hydrogen bond with IDO1, and π−π stacking interaction with TDO. IDO1/TDO-IN-4 can be used in the research of depression, and depression-induced infectious, metabolic, and autoimmune disorders.

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

IDO1/TDO-IN-4 Chemical Structure

IDO1/TDO-IN-4 Chemical Structure

CAS No. : 461424-21-5

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Based on 1 publication(s) in Google Scholar

IDO1/TDO-IN-4 Related Antibodies

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Description

IDO1/TDO-IN-4 is a potent IDO1/TDO dual inhibitor, with IC50 values of 3.53 μM (IDO1) and 1.15 μM (TDO). IDO1/TDO-IN-4 forms hydrogen bond with IDO1, and π−π stacking interaction with TDO. IDO1/TDO-IN-4 can be used in the research of depression, and depression-induced infectious, metabolic, and autoimmune disorders[1].

IC50 & Target[1]

IDO1

3.53 μM (IC50)

In Vitro

IDO1/TDO-IN-4 (compound 28, 0-2 μM, 1 h) inhibits the LPS-induced activation of BV2 microglial cells (determined by morphological changes)[1].
IDO1/TDO-IN-4 (0-2 μM, 1 h) inhibits the generation of pro-inflammatory factors and promotes the expression of IL-10[1].
IDO1/TDO-IN-4 (0-2 μM, 1 h) decreases the expression of IDO1 and prevents the excessive degradation of tryptophan via the kynurenine pathway[1].

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

IDO1/TDO-IN-4 Related Antibodies

RT-PCR[1]

Cell Line: 100 ng/mL LPS-induced BV2 microglial cells
Concentration: 0, 0.25, 0.5, 1, 2 μM
Incubation Time: 1 h
Result: Inhibited the generation of COX2, iNOS, TNF-α, and IL-1β.
Increased the level of IL-10.
In Vivo

IDO1/TDO-IN-4 (compound 28, i.p., 20 mg/kg, at day 1, 2, 3) rescues LPS-induced neuroinflammation and depressive-like behavior in mice[1].
IDO1/TDO-IN-4 (I.p. or i.v., 20 mg/kg) displays high exposure and a high volume of distribution at the steady state in normal mice[1].

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

Animal Model: 2 mg/kg LPS-induced depressive mice[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection (i.p.), at day 1, 2, 3.
Result: Attenuated microglial activation significantly.
Decreased inflammatory factors in the hippocampus, such as TNF-α, IL-1β, and iNOS.
Downregulated LPS-induced overexpression of IDO1.
Animal Model: Male C57BL/6J mice (pharmacokinetic assay)[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection and intravenous injection
Result: Pharmacokinetic profile of IDO1/TDO-IN-4 (compound 28)
pharmacokinetic property T1/2 (h) Tmax (h) Cmax (ng/mL) bioavailability F (%)
i.v./i.p. 2.31/0.77 0.25 5543.99/3878 52.55
Molecular Weight

234.26

Formula

C14H10N4
CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

C12=CC=CC=C1NC3=C2C=CN=C3C4=CNC=N4
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 : 125 mg/mL (533.60 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Methanol : 16.67 mg/mL (71.16 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2688 mL 21.3438 mL 42.6876 mL
5 mM 0.8538 mL 4.2688 mL 8.5375 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (8.88 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 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 (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Methanol / DMSO 1 mM 4.2688 mL 21.3438 mL 42.6876 mL 106.7190 mL
5 mM 0.8538 mL 4.2688 mL 8.5375 mL 21.3438 mL
10 mM 0.4269 mL 2.1344 mL 4.2688 mL 10.6719 mL
15 mM 0.2846 mL 1.4229 mL 2.8458 mL 7.1146 mL
20 mM 0.2134 mL 1.0672 mL 2.1344 mL 5.3360 mL
25 mM 0.1708 mL 0.8538 mL 1.7075 mL 4.2688 mL
30 mM 0.1423 mL 0.7115 mL 1.4229 mL 3.5573 mL
40 mM 0.1067 mL 0.5336 mL 1.0672 mL 2.6680 mL
50 mM 0.0854 mL 0.4269 mL 0.8538 mL 2.1344 mL
60 mM 0.0711 mL 0.3557 mL 0.7115 mL 1.7787 mL
DMSO 80 mM 0.0534 mL 0.2668 mL 0.5336 mL 1.3340 mL
100 mM 0.0427 mL 0.2134 mL 0.4269 mL 1.0672 mL
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IDO1/TDO-IN-4 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:

IDO1/TDO-IN-4461424-21-5Indoleamine 2,3-Dioxygenase (IDO)Antidepressiondepressioninflammationkynurenine pathwayBV2neuroinflammationLPSInhibitorinhibitorinhibit

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