Antitubercular agent-32
Antitubercular agent-32 is a derivate of Benzothiazinone (HY-13579A), inhibits M. tuberculosis, and shows improved metabolic stability and enhanced water solubility. Antitubercular agent-32 exerts antitubercular effect by targeting decaprenylphosphoryl-β-D-ribose 2’-oxidase (DprE1, IC50=3.9 μM).
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- CAS No.: 2498762-42-6
- Formule: C22H28N4O5S2
- Masse moléculaire:492.61
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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
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Activité biologique
Description
In Vitro
Antitubercular agent-32 (compound 8) (0-7.5 mg/mL; 48 h) shows low cytotoxicity and inhibits M. tuberculosis H37Rv with the minimum inhibition concentration (MIC) of 40 nM[1].
Antitubercular agent-32 (0-20 μM) inhibits decaprenylphosphoryl-β-D-ribose 2’-oxidase (DprE1, 0.5 μM), an enzyme essential for the biosynthesis of mycobacterial cell wall, with an IC50 value of 3.9 μM[1].
Antitubercular agent-32 (1 μM; 10 min) exhibits metabolic stability in the liver microsomal metabolic of both human (HLM) and mouse (MLM), with fast clearance rates of 77 mL/min/kg (HLM) and 163 mL/min/kg (MLM), respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HepG2 cells
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Concentration:0, 15, 30, 75, 150, 300, 750, 1500, 3000, and 7500 ng/mL
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Incubation Time:48 hours
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Result:There were no significantly growth inhibitions of HepG2 cells.
Chemical Information
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CAS No. 2498762-42-6
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Masse moléculaire 492.61
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Formule C22H28N4O5S2
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SMILES
CS(=O)(C(C=C12)=CC([N+]([O-])=O)=C1SC(N(CCN3CC4CCCCC4)CC53CC5)=NC2=O)=O
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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.
Protocole
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antitubercular agent-32 Related Classifications
HY-151340 Related Classifications
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