IDO1/TDO-IN-12
IDO1/TDO-IN-12 is an IDO1/TDO2 inhibitor with IC50 values of 0.825 and 4.04 μM, respectively. IDO1/TDO-IN-12 interacts with the ferrous heme cofactor in IDO1 as a non-competitive tryptophan inhibitor. IDO1/TDO-IN-12 inhibits nitric oxide production in LPS (HY-D1056)-stimulated immune cells. IDO1/TDO-IN-12 relieves pulmonary edema and lung injury in LPS-induced mouse models. IDO1/TDO-IN-12 can be used for the research of acute lung injury (ALI).
For research use only. We do not sell to patients.
- CAS No.: 2841468-09-3
- Formula: C19H17ClF3N3O5S2
- Molecular Weight:523.93
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
IDO1 0.825 μM (IC50) |
TNF-α |
IL-1β |
In Vitro
IDO1/TDO-IN-12 (compound 22) (48 h) inhibits IDO1 activity in IFN-γ-stimulated BxPC-3 cells with an IC50 of 0.854 μM[1].
IDO1/TDO-IN-12 (0.05-5.0 μM; 48 h) inhibits LPS-induced NO production in RAW264.7 cells in a concentration-dependent manner, with 31.3%, 40.2%, and 78.1% inhibition at 0.05, 0.5, and 5.0 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
response and lung injury in a mouse model of ALI[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (male, 8 weeks old) with LPS-induced acute lung injury)[1]
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Dosage:15; 50; 100 mg/kg
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Administration:i.p.; two doses; 0.5 h pre-LPS and 12 h post-LPS
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Result:Significantly reduced pulmonary edema (lung wet/dry ratio) compared to LPS-only group, with no dose-dependent reduction observed.
Reduced lung tissue levels of TNF-α and IL-1β in a dose-dependent manner.
Protected against lung injury in a dose-dependent manner based on H&E staining lung injury scoring.
Reduced lung tissue expression of myeloperoxidase (MPO) and citrullinated histone H3 (CitH3) in a dose-dependent manner.
Caused no significant changes in mouse body weight across any treatment groups.
Chemical Information
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CAS No. 2841468-09-3
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Molecular Weight 523.93
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Formula C19H17ClF3N3O5S2
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SMILES
O=C(C1=CC2=C(OC(S(CC3=CC=C(C=C3)Cl)=O)=N2)C=C1)NCCCNS(=O)(C(F)(F)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Inhalation Toxicity Study
Inhalation toxicity studies expose rodents to a controlled aerosol, vapor, gas, or smoke atmosphere and assess respiratory and systemic toxicity using exposure-atmosphere characterization, clinical observations, body and organ weights, bronchoalveolar lavage fluid, histopathology, blood chemistry, hematology, and, when included, molecular endpoints such as transcriptomics, proteomics, lipidomics, or tissue burden analysis. The primary biological readouts are airway irritation, pulmonary inflammation, cytotoxicity, altered surfactant or lipid homeostasis, impaired particle clearance, and tissue remodeling, reflected by BALF cell differentials, BALF protein, LDH, phosphatase activities, cytokines, lung weight, microscopic respiratory-tract lesions, and retained lung burden.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IDO1/TDO-IN-12 Related Classifications
HY-184027 Related Classifications
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