DNDI-8219
DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.
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- CAS No.: 2222660-40-2
- Formule: C13H10F3N3O5
- Masse moléculaire:345.23
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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Trypanosoma |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L6 | IC50 |
>100 μM
Compound: 58
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Cytotoxicity against rat L6 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
Cytotoxicity against rat L6 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
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[PMID: 33007723] |
| MRC5 | IC50 |
>64 μM
Compound: R-6
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Cytotoxicity against human MRC5 cells after 72 hrs by resazurin dye based assay
Cytotoxicity against human MRC5 cells after 72 hrs by resazurin dye based assay
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[PMID: 29461823] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice (infected with T. cruzi; n=5)[1]
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Dosage:50 or 100 mg/kg
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Administration:PO; once daily for five days
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Result:Completely cured one of five mice in a chronic infection mouse model, as well as markedly reduced parasite burdens in two other mice.
Chemical Information
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CAS No. 2222660-40-2
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Masse moléculaire 345.23
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Formule C13H10F3N3O5
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SMILES
FC(F)(F)OC1=CC=C(O[C@@H]2CN3C(OC2)=NC([N+]([O-])=O)=C3)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DNDI-8219 Related Classifications
HY-124623 Related Classifications
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