化学信息：
|
化学名
|
1-(6-bromo-2-methoxyquinolin-3-yl)-4-(dimethylamino)-2-naphthalen-1-yl-1-phenylbutan-2-ol
|
|
|
简称
|
Bedaquiline
|
|
别名
|
Sirturo, TMC207, R207910, TMC 207, R 207910, TMC-207, R-207910
|
|
中文名
|
贝达喹啉
|
|
化学式
|
C32H31BrN2O2
|
|
分子量
|
555.5
|
|
CAS号
|
843663-66-1
|
|
纯度
|
98%
|
|
溶剂/溶解度
|
Water<1mg/ml; DMSO6mg/ml; Ethanol<1mg/ml
|
|
溶液配制
|
5mg加入0.9ml DMSO，或者每5.56mg加入1ml DMSO，配制成10mM溶液。SC3251-10mM用DMSO配制。
|
生物信息：
|
产品描述
|
Bedaquiline(TMC207; R207910) is an anti-tuberculosis drug which selectively inhibit the mycobacterial energy metabolism i.e. ATP synthesis and found to be effective against all states of Mycobacterium tuberculosis.
|
|
信号通路
|
Anti-infection
|
|
靶点
|
anti-TB
|
－
|
－
|
－
|
－
|
|
IC50
|
－
|
－
|
－
|
－
|
－
|
|
体外研究
|
Preclinical studies have shown the efficacy of bedaquiline in terms of reduction in bacterial load and treatment duration. Phase II clinical studies have established the safety, tolerability and earlier sputum conversion time in patients with MDR-TB. In 2012 FDA approved bedaquiline for treatment of MDR-TB and XDR-TB. Bedaquiline possesses a unique mechanism of action that disrupts the activity of the mycobacterial adenosine triphosphate synthase. Clinical trials have been conducted evaluating the use of bedaquiline in combination with a background regimen for the treatment of adults with pulmonary MDR-TB. Bedaquiline has an excellent in vitro activity against Mycobacterium tuberculosis, including multidrug resistant M tuberculosis; however, its side effect profile limits its use against MDR-TB when no other effective regimen can be provided.
|
|
体内研究
|
N/A
|
|
临床实验
|
N/A
|
|
特征
|
N/A
|
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
|
酶活性检测实验
|
|
方法
|
N/A
|
|
细胞实验
|
|
细胞系
|
N/A
|
|
浓度
|
N/A
|
|
处理时间
|
N/A
|
|
方法
|
N/A
|
|
动物实验
|
|
动物模型
|
N/A
|
|
配制
|
N/A
|
|
剂量
|
N/A
|
|
给药方式
|
N/A
|
参考文献：
1. Lakshmanan M, et al. J Young Pharm. 2013 Dec, 5(4), 112-115.
2. Chahine EB, et al. Ann Pharmacother. 2014 Jan, 48(1), 107-15.
包装清单：
|
产品编号
|
产品名称
|
包装
|
|
SC3251-10mM
|
Bedaquiline (抗结核分枝杆菌)
|
10mM×0.2ml
|
|
SC3251-5mg
|
Bedaquiline (抗结核分枝杆菌)
|
5mg
|
|
SC3251-25mg
|
Bedaquiline (抗结核分枝杆菌)
|
25mg
|
|
—
|
说明书
|
1份
|
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
微信在线咨询
微信在线咨询
