TBA-354

• Description :

  TBA-354 is a potent anti-tuberculosis compound; maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains. IC50 value: Target: Anti-tuberculosis agent in vitro: TBA-354 is narrow spectrum and bactericidal in vitro against replicating and nonreplicating Mycobacterium tuberculosis, with potency similar to that of delamanid and greater than that of PA-824. TBA-354 maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates [1]. TBA-354 is 5 to 10 times more potent than PA-824, but selected mutants are cross-resistant to PA-824 and delamanid. TBA-354 is 2 to 4 times more potent than PA-824 when combined with bedaquiline, and when administered at a dose equivalent to that of PA-824, TBA-354 demonstrated superior sterilizing efficacy [2]. in vivo: TBA-354 has high bioavailability and a long elimination half-life. In vitro studies suggest a low risk of drug-drug interactions. Low-dose aerosol infection models of acute and chronic murine tuberculosis reveal time- and dose-dependent in vivo bactericidal activity that is at least as potent as that of delamanid and more potent than that of PA-824.

• UNSPSC :

  12352005

• Target :

  Antibiotic; Bacterial

• Type :

  Reference compound

• Related Pathways :

  Anti-infection

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Infection

• Assay Protocol :

  https://www.medchemexpress.com/TBA-354.html

• Purity :

  99.74

• Solubility :

  DMSO : 100 mg/mL (ultrasonic)

• Smiles :

  FC(F)(F)OC1=CC=C(C2=CC=C(CO[C@H]3CN4C(OC3)=NC([N+]([O-])=O)=C4)C=N2)C=C1

• Molecular Formula :

  C19H15F3N4O5

• Molecular Weight :

  436.34

• References & Citations :

  [1]Upton AM, et al. In Vitro and In Vivo Activities of the Nitroimidazole TBA-354 against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2015 Jan;59 (1) :136-44.|[2]Tasneen R, et al. Contribution of the Nitroimidazoles PA-824 and TBA-354 to the Activity of Novel Regimens in Murine Models of Tuberculosis. Antimicrob Agents Chemother. 2015 Jan;59 (1) :129-35.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 1

• CAS Number :

  [1257426-19-9]