Bedaquiline

Catalog No.S5623 Batch:S562301

Technical Data

Formula	C₃₂H₃₁BrN₂O₂
Molecular Weight	555.50	CAS No.	843663-66-1
Solubility (25°C)*	In vitro	DMSO	12 mg/mL (21.6 mM)
		Ethanol	3 mg/mL (5.4 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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].

In vivo

Bedaquiline follows triphasic elimination and characterized by an outstandingly long terminal half-life, around 173 h in humans^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	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.

Cell Assay:^{^[1]}

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.

References

Selleck's Bedaquiline has been cited by 5 publications

Near-field sensor array with 65-GHz CMOS oscillators can rapidly and comprehensively evaluate drug susceptibility of Mycobacterium [ Sci Rep, 2023, 13(1):3825]	PubMed: 36882499
Wollamide Cyclic Hexapeptides Synergize with Established and New Tuberculosis Antibiotics in Targeting Mycobacterium tuberculosis [ Microbiol Spectr, 2023, e0046523.]	PubMed: 37289062
Nano-in-Microparticles for Aerosol Delivery of Antibiotic-Loaded, Fucose-Derivatized, and Macrophage-Targeted Liposomes to Combat Mycobacterial Infections: In Vitro Deposition, Pulmonary Barrier Interactions, and Targeted Delivery [ Adv Healthc Mater, 2022, e2102117]	PubMed: 35112802
Activity of Drug Combinations against Mycobacterium abscessus Grown in Aerobic and Hypoxic Conditions [ Microorganisms, 2022, 10(7)1421]	PubMed: 35889140
Effects of Bedaquiline on Antimicrobial Activity and Cytokine Secretion of Macrophages Infected with Multidrug-Resistant Mycobacterium tuberculosis Strains [ Can J Infect Dis Med Microbiol, 2022, 2022:2703635]	PubMed: 35449601

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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