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Bedaquiline
Bedaquiline is a diarylquinoline drug and inhibits Mycobacterium tuberculosis F1FO-ATP synthase by simultaneously targeting the subunit c and subunit ε. Bedaquiline has uncoupling activity and is used for the multi-drug resistant tuberculosis[1].?
Bedaquiline has anticancer activity against cancer stem cell-like cells. Bedaquiline treatment of MCF7 breast cancer cells can inhibit mitochondrial oxygen consumption and glycolysis, but can induce oxidative stress. Bedaquiline can reduce mitochondrial membrane potential and significantly increase ROS levels[2].?
Bedaquiline follows the principle of three-stage elimination, and its terminal half-life is very long, approximately 173 hours in humans[3].?
References:
[1]. Jang J C, Jung Y G, Choi J, et al. Bedaquiline susceptibility test for totally drug-resistant tuberculosisMycobacterium tuberculosis. Journal of Microbiology, 2017, 55(6): 483-487.
[2]. Fiorillo M, Lamb R, Tanowitz H, et al. Bedaquiline, an FDA-approved antibiotic, inhibits mitochondrial function and potently blocks the proliferative expansion of stem-like cancer cells (CSCs). Aging, 2016, 8(8): 1593-1607.
[3]. Lakshmanan M, Xavier A S. Bedaquiline–The first ATP synthase inhibitor against multi drug resistant tuberculosis. Journal of Young Pharmacists, 2013, 5(4): 112-115.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 525.5 |
Cas No. | 843663-66-1 |
Formula | C31H29BrN2O |
Solubility | ≥22.05 mg/mL in DMSO with gentle warming; insoluble in EtOH; insoluble in H2O |
Chemical Name | (1R,2S)-1-(6-bromoquinolin-3-yl)-4-(dimethylamino)-2-(naphthalen-1-yl)-1-phenylbutan-2-ol |
SDF | Download SDF |
Canonical SMILES | CN(C)CC[C@@]([C@H](C1=CC=CC=C1)C2=CC3=CC(Br)=CC=C3N=C2)(O)C4=CC=CC5=C4C=CC=C5 |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment:[1] | |
Cell lines |
MCF-7 human breast cancer cells |
Reaction Conditions |
48 h incubation |
Applications |
Bedaquiline treatment (10 μM) of MCF-7 breast cancer cells inhibited mitochondrial oxygen-consumption, as well as glycolysis, but induced oxidative stress. Importantly, bedaquiline significantly blocked the propagation and expansion of MCF-7-derived cancer stem cells, with an IC50 value of ~ 1 μM. |
Animal experiment:[2] | |
Animal models |
Mice infected with Mycobacterium tuberculosis (M. tuberculosis) |
Dosage form |
25 mg/kg Administered orally, 5 days per week, for 14 weeks |
Applications |
The bedaquiline-containing regimen (rifampicin, isoniazid, pyrazinamide and bedaquiline) achieved total organ cfu count clearance at 8 weeks after treatment initiation, faster than the standard regimen consisting of rifampicin, isoniazid, pyrazinamide and ethambutol (14 weeks). Furthermore, the bedaquiline-containing regimen removed culture filtrate-dependent persistent bacilli at 8 weeks, leading to no disease relapse. |
Note |
The technical data provided above is for reference only. |
References: 1. 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. 2. Hu Y, Pertinez H, Liu Y, et al. Bedaquiline kills persistent Mycobacterium tuberculosis with no disease relapse: an in vivo model of a potential cure. Journal of Antimicrobial Chemotherapy, 2019, 74(6): 1627-1633. |
Quality Control & MSDS
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