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Bedaquiline

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Chemical Structure| 843663-66-1 同义名 : R207910;TMC207
CAS号 : 843663-66-1
货号 : A193466
分子式 : C32H31BrN2O2
纯度 : 99%+
分子量 : 555.5
MDL号 : MFCD14635354
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(21.6 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Bedaquiline is a mycobacterial adenosine triphosphate (ATP) synthase inhibitor that selectively inhibits the energy metabolism of Mycobacterium tuberculosis and many non-tuberculous mycobacteria.[3] Bedaquiline at 1 and 10μM inhibited oxygen consumption in MCF7 breast cancer cells in a dose-dependent manner. Bedaquiline at a dose of 10μM inhibited glycolysis and reduced mitochondrial membrane potential in MCF7 cells at 48-h post-treatment. Bedaquiline at the same dose augmented oxygen consumption and glycolysis in normal human fibroblasts. Additionally, bedaquiline inhibited the propagation of the cancer stem-like cells with an IC50 value of ~1μM.[4] In a murine model of tuberculosis, animals treated with 25mg/kg bedaquiline along with isoniazid, rifampicin, and pyrazinamide for six weeks showed lung culture negativity for AFB.[3]
作用机制 Bedaquiline is a diarylquinoline anti-tuberculosis that binds to the c subunit of the ATP synthase complex, blocks the rotation of the discs, thereby inhibiting the process of ATP synthase.[3]
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00042289 HIV Infections Phase 4 Recruiting September 30, 2019 -
NCT03625739 - Recruiting December 31, 2026 China ... 展开 >> Beijing Children's Hospital of Capital Medical University Recruiting Beijing, China Contact: Adong Shen, Master    13370115087    shenad16@hotmail.com 收起 <<
NCT03237182 Tuberculosis, Multidrug-Resist... 展开 >>ant 收起 << Phase 4 Recruiting December 2021 South Africa ... 展开 >> King Dinuzulu Hospital Recruiting Durban, Kwa-Zulu Natal, South Africa Contact: Nesri Padayatchi, MBcHB    0312604550    nesri.padayatchi@caprisa.org    Contact: Resha Boodhram, BTech    0828383651    resha.boodhram@caprisa.org 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.00mL

1.80mL

0.90mL

18.00mL

3.60mL

1.80mL
参考文献

[1]Jang JC, Jung YG, et al. Bedaquiline susceptibility test for totally drug-resistant tuberculosis Mycobacterium tuberculosis. J Microbiol. 2017 Jun;55(6):483-487.

[2]Chahine EB, Karaoui LR, et al. Bedaquiline: a novel diarylquinoline for multidrug-resistant tuberculosis. Ann Pharmacother. 2014 Jan;48(1):107-15.

[3]Lakshmanan M, Xavier AS. Bedaquiline - The first ATP synthase inhibitor against multi drug resistant tuberculosis. J Young Pharm. 2013;5(4):112-115. doi:10.1016/j.jyp.2013.12.002

[4]Fiorillo M, Lamb R, Tanowitz HB, et al. Bedaquiline, an FDA-approved antibiotic, inhibits mitochondrial function and potently blocks the proliferative expansion of stem-like cancer cells (CSCs). Aging (Albany NY). 2016;8(8):1593-1607. doi:10.18632/aging.100983