TBAJ-587 是一种有效的抗结核药物，在 MABA 和 LORA 实验中抑制 M.tb 菌株 H37Rv 生长 MIC90 分别为 0.006 和<0.02 μg/mL。TBAJ-587 对 hERG 通道的抑制作用很低，大大减弱了对心脏钾通道蛋白的抑制，这对心脏复极化很重要。
货号:ajcx39450
CAS:2252316-16-6
分子式:C30H33BrFN3O5
分子量：614.5
溶解度:DMSO : 43.33 mg/mL (70.51 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

[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.