化学信息：
|
化学名
|
(6S)-2-nitro-6-[[6-[4-(trifluoromethoxy)phenyl]pyridin-3-yl]methoxy]-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine
|
|
|
简称
|
TBA-354
|
|
别名
|
SN31354, TBA354, TBA 354
|
|
中文名
|
N/A
|
|
化学式
|
C19H15F3N4O5
|
|
分子量
|
436.34
|
|
CAS号
|
1257426-19-9
|
|
纯度
|
98%
|
|
溶剂/溶解度
|
Water<1mg/ml; DMSO5mg/ml; Ethanol<1mg/ml
|
|
溶液配制
|
5mg加入1.15ml DMSO，或者每4.36mg加入1ml DMSO，配制成10mM溶液。SC3319-10mM用DMSO配制。
|
生物信息：
|
产品描述
|
TBA-354 is a potent anti-tuberculosis compound; maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates.
|
|
信号通路
|
Anti-infection
|
|
靶点
|
Anti-tuberculosis
|
－
|
－
|
－
|
－
|
|
IC50
|
－
|
－
|
－
|
－
|
－
|
|
体外研究
|
TBA-354 is narrow spectrum and bactericidal in vitro against replicating and nonreplicating Mycobacterium tuberculosis, with potency similar to that of delamanid and greater than that of PA-824. TBA-354 maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates. TBA-354 is 5 to 10 times more potent than PA-824, but selected mutants are cross-resistant to PA-824 and delamanid. TBA-354 is 2 to 4 times more potent than PA-824 when combined with bedaquiline, and when administered at a dose equivalent to that of PA-824, TBA-354 demonstrated superior sterilizing efficacy.
|
|
体内研究
|
TBA-354 has high bioavailability and a long elimination half-life. In vitro studies suggest a low risk of drug-drug interactions. Low-dose aerosol infection models of acute and chronic murine tuberculosis reveal time- and dose-dependent in vivo bactericidal activity that is at least as potent as that of delamanid and more potent than that of PA-824.
|
|
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. Upton AM, et al. Antimicrob Agents Chemother. 2015 Jan, 59(1), 136-44.
2. Tasneen R, et al. Antimicrob Agents Chemother. 2015 Jan, 59(1), 129-35.
包装清单：
|
产品编号
|
产品名称
|
包装
|
|
SC3319-10mM
|
TBA-354 (抗结核)
|
10mM×0.2ml
|
|
SC3319-5mg
|
TBA-354 (抗结核)
|
5mg
|
|
SC3319-25mg
|
TBA-354 (抗结核)
|
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
