Bedaquiline是一种二芳基喹啉药物，能同时靶向 c-亚基和 ε-亚基，抑制结核分枝杆菌 (Mtb) F1FO-ATP合酶。它具有解偶联活性和有用于耐多药结核病的潜力。

Bedaquiline(TMC207; R207910) is an anti-tuberculosis drug which selectively inhibit the mycobacterial energy metabolism i.e. ATP synthesis and found to be effective against all states of Mycobacterium tuberculosis.

Bedaquiline inhibits the growth of TDR M. tuberculosis strains, with MIC values ranging from 0.125 to 0.5 mg/L[1]. Among slowly growing mycobacteria (SGM), bedaquiline exhibits the highest activity against Mycobacterium avium with MIC50 and MIC90 values of 0.03 and 16 mg/L, respectively. Among rapidly growing mycobacteria (RGM), Mycobacterium abscessus subsp. abscessus (M. abscessus) and Mycobacterium abscessus subsp. massiliense (M. massiliense) seem more susceptible to bedaquiline than Mycobacterium fortuitum, with MIC50 and MIC90 values of 0.13 and >16 mg/L, respectively, for both species. Bedaquiline also shows moderate in vitro activity against NTM species[2]. Bedaquiline has an excellent in vitro activity against Mycobacterium tuberculosis, including multidrug resistant M tuberculosis[3].

843663-66-1

C32H31BrN2O2

555.516

TMC207;贝达喹啉;R207910

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years