Antitubercular agent-56
Antitubercular agent-56, a Questiomycin A (HY-N8439) derivative, is a potent and orally active antitubercular agent. Antitubercular agent-56 disrupts mycobacterial envelope integrity by inhibiting FabD (Kd = 9.39 μM; IC50 = 49.60 μM). Antitubercular agent-56 exhibits good intracellular antimycobacterial activity against Mycobacterium tuberculosis (MTB) and drug-resistant MTB both in vitro and in vivo. Antitubercular agent-56 can be used for research on tuberculosis (TB).
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- Fòrmula: C16H13N3O3
- Peso molecular:295.29
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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FabD 9.39 μM (Kd) |
FabD 49.60 μM (IC50) |
Antitubercular agent-56 (compound B10) (7 days) exhibits potent antitubercular activity against MTB H37Rv (MIC = 0.15 μg/mL) and drug-sensitive and drug-resistant MTB strains with MIC range from 0.063 to 0.25 μg/mL)[1].
Antitubercular agent-56 (0.26-64 μg/mL, 48 h) exhibits low cytotoxicity against Vero, HepG2 and J774A.1 cells with IC50s of >128, >80, and >80 μg/mL, respectively[1].
Antitubercular agent-56 (1/2 × MIC-16 × MIC; 0-14 days) exhibits potent bactericidal efficacy against H37Rv MTB strain and clinical isolate in a concentration- and time-dependent manner[1].
Antitubercular agent-56 (1-4 μg/mL; 72 h) effectively penetrates macrophages and inhibits intracellular MTB growth[1].
Antitubercular agent-56 (4 × MIC; 30 min) significantly increases mycobacterial membrane permeability compared to control, confirming its disruptive effect on cell wall integrity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-24 |
|---|---|---|---|---|---|---|
| Mice[1] | 10 nM | p.o. | 5.34 h | 0.5 h | 229.97 ng/mL | 738.12 ng·h/mL |
Antitubercular agent-56 (500 mg/kg; i.g.; single dose) exhibits a favorable safety profile in mice[1].
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 (18-20 g) infected with Mycobacterium tuberculosis H37Ra strain[1]
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Dosage:100 mg/kg
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Administration:i.g.; five times weekly for 3 weeks
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Result:Induced little reductions in mean lung bacterial burden, demonstrating log10 CFU decreases of 0.84.
Showed inhibitory activity against Mycobacterium tuberculosis H37Ra.
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Animal Model:Female BALB/c mice (17-20 g)[1]
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Dosage:500 mg/kg
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Administration:i.g.; single dose
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Result:Showed all mice survived without any abnormalities compared to control.
Showed no significant changes in body weight.
Chemical Information
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Peso molecular 295.29
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Fòrmula C16H13N3O3
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SMILES
O=C1C(NC(NC2CC2)=O)=CC3=NC4=C(OC3=C1)C=CC=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antitubercular agent-56 Related Classifications
HY-181008 Related Classifications
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