Catalog No.S5623 Synonyms: TMC-207, R207910
Molecular Weight(MW): 555.50
Bedaquiline, a diarylquinoline, binds to subunit c of mycobacterial ATP synthase and inhibits its activity. It is highly selective for mycobacterial ATP synthase enzyme compared to homologous eukaryotic enzyme (Selectivity Index >20 000).
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|Description||Bedaquiline, a diarylquinoline, binds to subunit c of mycobacterial ATP synthase and inhibits its activity. It is highly selective for mycobacterial ATP synthase enzyme compared to homologous eukaryotic enzyme (Selectivity Index >20 000).|
Bedaquiline targets against Mycobacterial ATP synthase complex. Bedaquiline has anti-cancer activity, directed against Cancer Stem-like Cells (CSCs). Bedaquiline treatment of MCF7 breast cancer cells inhibits mitochondrial oxygen-consumption, as well as glycolysis, but induces oxidative stress. Bedaquiline reduces mitochondrial membrane potential, with a significant rise in ROS levels. It specifically inhibits mitochondrial respiration in cancer cells, while enhancing mitochondrial function in normal cells. Bedaquiline dramatically inhibits oxygen consumption and ATP production in the low micromolar range. In addition, bedaquiline treatment also reduced aerobic glycolysis.
|In vivo||Bedaquiline follows triphasic elimination and characterized by an outstandingly long terminal half-life, around 173 h in humans.|
|In vitro||DMSO||12 mg/mL (21.6 mM)|
|Ethanol||3 mg/mL (5.4 mM)|
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