TBAJ-587

Names

[ Name ]:
TBAJ-587

Biological Activity

[Description]:

TBAJ-587, a potent anti-tuberculosis agent, inhibits M.tb strain H37Rv growth with MIC90s of 0.006 and <0.02 µg/mL in MABA and LORA assay, respectively. TBAJ-587 inhibits hERG channel minimally, attenuates inhibition of the cardiac potassium channel protein coded by the hERG, which is important for cardiac repolarization[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

[Target]

Anti-tuberculosis[1]

[In Vitro]

Bedaquiline is a drug of the diarylquinoline class that has proven to be clinically effective against drug-resistant tuberculosis, but has a cardiac liability due to its potent inhibition of the cardiac potassium channel protein hERG. TBAJ-587, an analogue of Bedaquiline, demonstrates more potent anti-tubercular activity, with greatly attenuated hERG blockade. TBAJ-587 inhibits hERG channel with an IC50 of 13 μM[1].

[References]

[1]. Sutherland HS, et al. 3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel. Bioorg Med Chem. 2019 Apr 1;27(7):1292-1307.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₀H₃₃BrFN₃O₅

[ Molecular Weight ]:
614.50

Related Compounds

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