产品
编 号：F753407
分子式：C22H28N4O5S2
分子量：492.61
分子式：C22H28N4O5S2
分子量：492.61
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CAS No: 2498762-42-6
产品详情
生物活性：
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).
体外研究：
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.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.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.
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).
体外研究：
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.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.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.
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