TMC207 (Bedaquiline) is a diarylquinoline-based inhibitor of bacterial ATP synthase at nanomolar concentrations. In vitro mycobacterial experiments show that TMC207 inhibits drug-sensitive and drug-resistant mycobacterial TB at an MIC range of 2 to 60 nM and an MIC50 of 30 ng/mL. Additionally TMC207 is broadly potent against many non-tuberculous mycobacteria, with MICs of 6 to 500 nM. (1)
Studies show that TMC207 is orally-available and efficacious on a once-daily administration for patients with pulmonary TB. No serious adverse events were observed. (2)
Technical information:
Chemical Formula: | C32H31BrN2O2 | |
CAS #: | 843663-66-1 | |
Molecular Weight: | 555.5 | |
Purity: | > 98% | |
Appearance: | white | |
Chemical Name: | (1R,2S)-1-(6-bromo-2-methoxyquinolin-3-yl)-4-(dimethylamino)-2-(naphthalen-1-yl)-1-phenylbutan-2-ol | |
Solubility: | Up to 2 mM in DMSO | |
Synonyms: | TMC207, TMC-207, Bedaquiline |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
1. | Matteelli et al., TMC207: the first compoudn of a new class of potent anti-tuberculosis drugs. Future Microbiol. 2010, 5(6), 849-858. Pubmed ID: 20521931 |
2. | Rustomjee et al., Early Bactericidal Activity and Pharmacokinetics of the Diarylquinoline TMC207 in Treatment of Pulmonary Tuberculosis. Antimicrob. Agents Chemother. 2008, 52(8), 2831-2835. Pubmed ID: 18505852 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.