Bedaquiline (Synonyms: 贝达喹啉; TMC207; R207910)
目录号: PL12279 纯度: ≥99%
CAS No. :843663-66-1
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中文名称
Bedaquiline
中文别名
6-溴-alpha-[2-(二甲基氨基)乙基]-2-甲氧基-alpha-1-萘基-beta-苯基-3-喹啉乙醇;贝达喹啉;(2-乙基己基)溴化镁, 1.0 M 乙醚溶液, J&KSeal瓶;6-溴-alpha-[2-(二甲基氨基)乙基]-2-甲氧基-alpha-1-萘基-beta;Bedaquiline标准品;TMC-207(Bedaquiline) 抑制剂;呗达喹啉;贝达喹林;贝达喹啉杂质;贝达喹啉杂质(Bedaquiline)对照品;贝达喹啉杂质对照品-标准品
英文名称
Bedaquiline
英文别名
(1R,2S)-1-(6-Bromo-2-methoxyquinolin-3-yl)-4-(dimethylamino)-2-(naphthalen-1-yl)-1-phenylbutan-2-ol;(αS,βR)-Bedaquiline;TMC 207;TMC-207;6-amino-2-benzamidohexanoic acid methyl ester hydrochloride;6-Bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol;Bedaquiline;BZ-LYS-OME HCL;methyl (2S)-6-amino-2-benzamidohexanoate;methyl 6-azanyl-2-benzamido-hexanoate hydrochloride;R207910;R-207910;BCP02829;AK145620;(2S)-1-(6-Bromo-2-methoxyquinolin-3-yl)-4-(dimethylamino)-2-naphthalen-1-yl-1-phenylbutan-2-ol
Cas No.
843663-66-1
分子式
C32H31BrN2O2
分子量
555.50
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Bedaquiline (TMC207) 是一种二芳基喹啉药物,通过同时靶向 c-亚基和 ε-亚基来抑制结核分枝杆菌 (Mtb) F1FO-ATP合酶。Bedaquiline 具有解偶联活性。Bedaquiline 有用于耐多药结核病的潜力。
生物活性
Bedaquiline (TMC207) is a diarylquinoline drug and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit. Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-drug resistant tuberculosis.
性状
Solid
IC50 & Target[1][2]
Mtb F1FO-ATP synthase
体外研究(In Vitro)
Bedaquiline inhibits the growth of TDR M. tuberculosis strains, with MIC values ranging from 0.125 to 0.5 mg/L. Among slowly growing mycobacteria (SGM), bedaquiline exhibits the highest activity against Mycobacterium avium with MIC50 and MIC90 values of 0.03 and 16 mg/L, respectively. Among rapidly growing mycobacteria (RGM), Mycobacterium abscessus subsp. abscessus (M. abscessus) and Mycobacterium abscessus subsp. massiliense (M. massiliense) seem more susceptible to bedaquiline than Mycobacterium fortuitum , with MIC50 and MIC90 values of 0.13 and >16 mg/L, respectively, for both species. Bedaquiline also shows moderate in vitro activity against NTM species. Bedaquiline has an excellent in vitro activity against Mycobacterium tuberculosis, including multidrug resistant M tuberculosis.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Jang JC, et al. Bedaquiline susceptibility test for totally drug-resistant tuberculosis Mycobacterium tuberculosis. J Microbiol. 2017 Apr 20.
[2]. Sarathy JP, et al. TBAJ-876 displays Bedaquiline-like mycobactericidal potency without retaining the parental drugs uncoupler activity. Antimicrob Agents Chemother. 2019 Nov 11.
溶解度数据
In Vitro: DMSO : 12.5 mg/mL (22.50 mM; ultrasonic and warming and heat to 60°C)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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