SML4007
TMC207
≥98% (HPLC)
别名:
(αS,βR)-6-Bromo-α-[2-(dimethylamino)ethyl]-2-methoxy-α-1-naphthalenyl-β-phenyl-3-quinolineethanol, (1R, 2S)-1-(6-Bromo-2methoxy-3-quinolinyl)-4-(dimethylamino)-2-(1-naphthalenyl)-1-phenyl-2-butanol, Bedaquiline, R 207910, R-207910, R207910
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所有图片(1)
About This Item
经验公式（希尔记法）:
C32H31BrN2O2
CAS号:
分子量:
555.50
MDL编号:
UNSPSC代码:
51111800
UNSPSC代码:
12352200
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质量水平
方案
≥98% (HPLC)
表单
powder
旋光性
[α]/D 195.0 to 155.0° (c = 0.5g/100mL in DMF)
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
BrC(C=C1)=CC2=C1N=C(OC)C([C@@H](C3=CC=CC=C3)[C@](O)(C4=CC=CC5=C4C=CC=C5)CCN(C)C)=C2
InChI key
QUIJNHUBAXPXFS-XLJNKUFUSA-N
生化/生理作用
Potent and selective mycobacterial ATP synthase inhibitor with broad-spectrum anti-mycobacterial activity.
TMC207 (Bedaquiline; R207910) is an orally active, potent and selective mycobacterial ATP synthase inhibitor (M. smegmatis IC50 = 2.5 nM or 1.4 ng (non-salt form)/mL; human mitochondrial ATP syntase IC50 >200 uM) with broad-spectrum anti-mycobacterial activity (MIC 10-120 ng/mL), including M. bovis, avium complex (MAC), kansasii, marinum, fortuitum, abscessus, smegmatis, ulcerans, and both drug-susceptible and multiple drug-resistant M. tuberculosis strains (to rigampin, isoniazid, streptomycin, ethambutol, pyrazinamide, fluoroquinolone).
TMC207 (Bedaquiline; R207910) is an orally active, potent and selective mycobacterial ATP synthase inhibitor (M. smegmatis IC50 = 2.5 nM or 1.4 ng (non-salt form)/mL; human mitochondrial ATP syntase IC50 >200 uM) with broad-spectrum anti-mycobacterial activity (MIC 10-120 ng/mL), including M. bovis, avium complex (MAC), kansasii, marinum, fortuitum, abscessus, smegmatis, ulcerans, and both drug-susceptible and multiple drug-resistant M. tuberculosis strains (to rigampin, isoniazid, streptomycin, ethambutol, pyrazinamide, fluoroquinolone).
警示用语：
Warning
危险声明
预防措施声明
危险分类
Aquatic Chronic 1
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
从最新的版本中选择一种：
分析证书(COA)
Lot/Batch Number
Baohong Ji et al.
Antimicrobial agents and chemotherapy, 50(4), 1558-1560 (2006-03-30)
As measured by a proportional bactericidal technique in the mouse footpad system, the bactericidal activity against Mycobacterium leprae of R207910 was equal to that of rifapentine, rifampin, or moxifloxacin and significantly greater than those of minocycline, PA-824, and linezolid. These
Anna C Haagsma et al.
Antimicrobial agents and chemotherapy, 53(3), 1290-1292 (2008-12-17)
The diarylquinoline TMC207 kills Mycobacterium tuberculosis by specifically inhibiting ATP synthase. We show here that human mitochondrial ATP synthase (50% inhibitory concentration [IC(50)] of >200 microM) displayed more than 20,000-fold lower sensitivity for TMC207 compared to that of mycobacterial ATP
Anil Koul et al.
Nature chemical biology, 3(6), 323-324 (2007-05-15)
The diarylquinoline R207910 (TMC207) is a promising candidate in clinical development for the treatment of tuberculosis. Though R207910-resistant mycobacteria bear mutations in ATP synthase, the compound's precise target is not known. Here we establish by genetic, biochemical and binding assays
Koen Andries et al.
Science (New York, N.Y.), 307(5707), 223-227 (2004-12-14)
The incidence of tuberculosis has been increasing substantially on a worldwide basis over the past decade, but no tuberculosis-specific drugs have been discovered in 40 years. We identified a diarylquinoline, R207910, that potently inhibits both drug-sensitive and drug-resistant Mycobacterium tuberculosis
M Ibrahim et al.
Antimicrobial agents and chemotherapy, 51(3), 1011-1015 (2006-12-21)
In previous studies, the diarylquinoline R207910 (also known as TMC207) was demonstrated to have high bactericidal activity when combined with first- or second-line antituberculous drugs. Here we extend the evaluation of R207910 in the curative model of murine tuberculosis by
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