Antitubercular agent-32 是一种Benzothiazinone 衍生物，能够抑制结核分枝杆菌M. tuberculosis，并具有代谢稳定性和良好水溶性。Antitubercular agent-32 能够靶向 decaprenylphosphoryl-β-D-ribose 2’-氧化酶 (DprE1,IC50=3.9 μM) 来行使抗结核作用。

Antitubercular agent-32 is a derivate of Benzothiazinone, 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, IC 50 =3.9 μM) [1].

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 IC 50 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]. Cell Cytotoxicity Assay [1] Cell Line: HepG2 cells Concentration: 0, 15, 30, 75, 150, 300, 750, 1500, 3000, and 7500 ng/mL Incubation Time: 48 hours Result: There were no significantly growth inhibitions of HepG2 cells.

2498762-42-6

C22H28N4O5S2

492.61

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years