2252316-16-6

2252316-16-6 structure

Name: TBAJ-587
Chemical Name: TBAJ-587
CAS Number: 2252316-16-6
Molecular Formula: C₃₀H₃₃BrFN₃O₅
Molecular Weight: 614.50
Catalog: Signaling Pathways Anti-infection Bacterial
Create Date: 2019-06-01 12:53:18
Modify Date: 2024-01-10 17:28:35
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].

Name	TBAJ-587

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.

Molecular Formula	C₃₀H₃₃BrFN₃O₅
Molecular Weight	614.50