Bedaquiline

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Bedaquiline

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

843663-66-1

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
5mg	电议
10mg	电议
50mg	电议

产品介绍

化学性质

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
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
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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.

试验操作

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 withMycobacterium 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.