Bedaquiline

製品コードS5623 バッチS562302

印刷

化学情報

Chemical Structure Synonyms TMC-207, R207910 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C32H31BrN2O2
分子量 555.50 CAS No. 843663-66-1
Solubility (25°C)* 体外 DMSO 20 mg/mL (36.0 mM)
Ethanol 10 mg/mL (18.0 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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).
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MCF-7 cells
濃度 1μM and 10 μM
反応時間 48 h
実験の流れ

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.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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