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).
For research use only. We do not sell to patients.
- Formula: C16H13N3O3
- Molecular Weight:295.29
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
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FabD 9.39 μM (Kd) |
FabD 49.60 μM (IC50) |
In Vitro
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. Further protocols information, click here.
Parmacokinetics
| 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 |
In Vivo
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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Molecular Weight 295.29
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Formula C16H13N3O3
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SMILES
O=C1C(NC(NC2CC2)=O)=CC3=NC4=C(OC3=C1)C=CC=C4
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antitubercular agent-56 Related Classifications
HY-181008 Related Classifications
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