TBA-354 (抗结核)

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。

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

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－

－

－

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

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

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

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说明书

1份