85-2074-73　［取扱停止］Mycobacterium Bactericide, TCA1 (Ethyl-(2-(benzo[d]thiazole-2-carboxamido)thiophene-3-carbonyl)carbamate, Ethyl-((2-((1,3-benzothiazol-2-ylcarbonyl)amino)-3-thienyl)carbonyl)carbamate, Mtb Inhibitor, Mycobacteria DprE1 Inhibitor, Mycobacteria MoeW Inhibitor) 25mg　217575

特徴

• A cell-permeable benzothiazolylthiophene that exhibits bactericidal activity against mycobacteria, including M. smegmatis, M. bovis GCG, and M. tuberculosis (MIC50 = 30, 40, and 10ng/mL, respectively, in biofilm medium; MIC50 = 4.5, 3, 0.19ug/mL, respectively, in 7H9 medium), but not E. coli, Staphylococcus aureus, or Pseudomonas aeruginosa, by simultaneously targeting DprE1 FAD-binding domain of DprE1/DprE2 required for Mycobacterium cell wall arabinan biosynthesis and the Mtb MoeW protein involved in the biosynthesis of MoCo, molybdenum cofactor indispensable for nitrate assimilation via MoCo-dependent enzymes. Either alone or used in combination, TCA1 is shown to greatly complement INH (Isoniazid) and RIF (Rifampicin) against both wt and drug-resistant Mtb cultures in vitro (1-7.5ug/mL) and in treating acute and chronic Mtb H37Rv infections in mice in vivo (10-100mg/kg p.o.) with no apparent host toxicity.
• Molecular Formula:C₁₆H₁₃N₃O₄S₂
• Primary Target:DprE1
• Secondary Target:MoeW
• Solubility:DMSO
• Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.