| 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].
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| Related Catalog |
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| Target |
Anti-tuberculosis[1]
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| 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].
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| 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.
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