NEU-4438
NEU-4438 is an antimalarial agent. NEU-4438 inhibits DNA synthesis, reduces AMPK-γ, and increases Clathrin heavy chain. NEU-4438 exhibits antiparasitic activity against Trypanosoma brucei. NEU-4438 reduces trypanosome tissue burden in a chronic HAT mouse model.
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- CAS No.: 2306305-57-5
- Formule: C24H26N8
- Masse moléculaire:426.52
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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 |
NEU-4438 (serial dilutions; 6 h, then 48 h in drug-free medium) induces delayed trypanocidality in bloodstream Trypanosoma brucei brucei Lister427 cells, with a DC50 of 334 nM after 6 h treatment followed by 48 h in drug-free medium[1].
NEU-4438 (150-1013 nM; 6 h) dose-dependently reduces AMPK-γ protein levels and increases clathrin heavy chain levels in bloodstream Trypanosoma brucei cells expressing Myc-tagged versions of these proteins, with maximal effects at 1013 nM (DC90) after 6 h treatment[1].
NEU-4438 (150 nM; 6 h, then 1 h EdU labeling) inhibits nuclear DNA synthesis in bloodstream Trypanosoma brucei brucei Lister427 cells, as shown by a reduction in EdU-positive cells and decreased nuclear EdU signal intensity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:bloodstream Trypanosoma brucei cells expressing Myc-tagged AMPK-γ and clathrin heavy chain
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Concentration:159 nM (DCC25); 1474 nM (DCC90)
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Incubation Time:6 h
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Result:Reduced AMPK-γ protein levels 0.54-fold at DCC25 and 0.86-fold at DCC90 compared to vehicle-treated cells.
Increased clathrin heavy chain levels 0.19-fold at DCC25 and 0.36-fold at DCC90 nM compared to vehicle-treated cells.
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Cell Line:bloodstream Trypanosoma brucei brucei Lister427 cells
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Concentration:150 nM
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Incubation Time:6 h
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Result:Increased the fraction of trypanosomes with one basal body (1BB) and decreased the proportion of cells with two basal bodies (2BB), with a statistically significant difference in population distribution compared to vehicle-treated cells (p = 2.8×10-2, Pearson’s Chi-square test).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss-Webster (Hsd:ND4) (female, 8-10 weeks old, 20-25 g, infected with 5×104 bioluminescent T. brucei AnTat1.1 AmLuc via inoculation)[1]
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Dosage:150 mg/kg (days 1-4 post-infection); 120 mg/kg (days 5-7 post-infection)
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Administration:daily; days 1-7 post-infection
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Result:Produced a 3.92-fold reduction in trypanosome tissue bioluminescence signal on day 3 post-infection (p = 6.8×10-3).
Reduced median total trypanosome tissue flux greater than 100-fold, with undetectable tissue infection in 3 out of 4 treated mice on day 7 post-infection.
Left detectable parasites in tissues of 2 out of 4 treated mice on day 14 post-infection.
Chemical Information
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CAS No. 2306305-57-5
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Masse moléculaire 426.52
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Formule C24H26N8
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SMILES
CN1CCN(C2=NC=C(C3=CC(N(C)C=C/4)=C(C=C3)C4=N\C5=NC=CN=C5)C=N2)CCC1
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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)
NEU-4438 Related Classifications
HY-125188 Related Classifications
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- NEU-4438
- 2306305-57-5
- NEU4438
- NEU 4438
- Parasite
- DNA/RNA Synthesis
- AMPK
- Clathrin
- nuclear DNA synthesis
- bloodstream Trypanosoma brucei brucei Lister427 cells
- transferrin endocytosis
- AMPK-γ
- chronic human African trypanosomiasis
- Trypanosoma brucei
- haptoglobin-hemoglobin endocytosis
- basal body maturation
- mouse model
- polypeptide synthesis
- Inhibitor
- inhibitor
- inhibit