IDO1/TDO-IN-4
Based on 1 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.74%
- CAS. Nr.: 461424-21-5
- Formel: C14H10N4
- Molecular Weight:234.26
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) IDO1/TDO-IN-4
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Biologische Aktivität
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IDO1 3.53 μM (IC50) |
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.
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Cell Line:100 ng/mL LPS-induced BV2 microglial cells
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Concentration:0, 0.25, 0.5, 1, 2 μM
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Incubation Time:1 h
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Result:Inhibited the generation of COX2, iNOS, TNF-α, and IL-1β.
Increased the level of IL-10.
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.
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Animal Model:2 mg/kg LPS-induced depressive mice[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection (i.p.), at day 1, 2, 3.
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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.
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Animal Model:Male C57BL/6J mice (pharmacokinetic assay)[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection and intravenous injection
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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
Chemical Information
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CAS. Nr. 461424-21-5
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Appearance Solid
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Molecular Weight 234.26
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Formel C14H10N4
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Color Yellow to brown
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SMILES
C12=CC=CC=C1NC3=C2C=CN=C3C4=CNC=N4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Fish Shellfish Immunol
Edwardsiella piscicida infection-induced tryptophan-kynurenine metabolic pathway impairs Th17 cells to drive intestinal inflammation in teleost. [Abstract]2025 May 16:163:110425. PMID: 40383498
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
Please enter the basic information of animal experiments:
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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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
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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