Home Transmembrane Transporters ATPase inhibitor Bedaquiline For research use only.

Bedaquiline

Synonyms: TMC-207, R207910

Bedaquiline (TMC-207, R207910), 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 Chemical Structure

Bedaquiline Chemical Structure

CAS No. 843663-66-1

Purity & Quality Control

Bedaquiline Related Products

Signaling Pathway

ATPase Signaling Pathways

ATPase Signaling Pathway

Biological Activity

Description Bedaquiline (TMC-207, R207910), 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).
Targets
mycobacterial ATP synthase [1]
In vitro
In vitro Bedaquiline targets against Mycobacterial ATP synthase complex[1]. 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[2].
Cell Research Cell lines MCF-7 cells
Concentrations 1μM and 10 μM
Incubation Time 48 h
Method

MCF7 cells were treated with 10μM bedaquiline for 48 hours. Vehicle alone (DMSO) control cells were processed in parallel. After 48 hours, cells were washed with PBS, and incubated with CM-H2DCFDA (diluted in PBS/CM to a final concentration of 1 μM) for 20 minutes at 37°C. All subsequent steps were performed in the dark. Cells were rinsed, harvested, and re-suspended in PBS/CM. Cells were then analyzed by flow cytometry.
In Vivo
In vivo Bedaquiline follows triphasic elimination and characterized by an outstandingly long terminal half-life, around 173 h in humans[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05175794 Recruiting
Drug Resistant Tuberculosis|MDR-TB|XDR-TB|Tuberculosis
Centre for the AIDS Programme of Research in South Africa|KNCV Tuberculosis Foundation|Amsterdam Institute for Global Health and Development|Ospedale San Raffaele|Foundation for Innovative New Diagnostics Switzerland|National Institute for Medical Research Tanzania|University of St Andrews|Global Alliance for TB Drug Development|Wits Health Consortium (Pty) Ltd|Institute of Human Virology Nigeria|Ethiopian Public Health Institute
 May 26 2022 --
NCT04239326 Completed
Tuberculosis Multidrug-Resistant
Foundation for Innovative New Diagnostics Switzerland
 April 16 2021 --

Chemical Information & Solubility

Molecular Weight 555.50 Formula

C32H31BrN2O2
CAS No. 843663-66-1 SDF --
Smiles CN(C)CCC(C1=CC=CC2=CC=CC=C21)(C(C3=CC=CC=C3)C4=C(N=C5C=CC(=CC5=C4)Br)OC)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 33 mg/mL ( (59.4 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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