化學名

(6S)-2-nitro-6-[[6-[4-(trifluoromethoxy)phenyl]pyridin-3-yl]methoxy]-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine

簡稱

TBA-354

別名

SN31354, TBA354, TBA 354

中文名

N/A

化學式

C₁₉H₁₅F₃N₄O₅

分子量

436.34

CAS號

1257426-19-9

純度

98%

溶劑/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。

產品描述

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.

信號通路

Anti-infection

靶點

Anti-tuberculosis

－

－

－

－

IC50

－

－

－

－

－

體外研究

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.

體內研究

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.

臨床實驗

N/A

特征

N/A

酶活性檢測實驗

方法

N/A

細胞實驗

細胞系

N/A

濃度

N/A

處理時間

N/A

方法

N/A

動物實驗

動物模型

N/A

配制

N/A

劑量

N/A

給藥方式

N/A

產品編號

產品名稱

包裝

SC3319-10mM

TBA-354 (抗結核)

10mM×0.2ml

SC3319-5mg

TBA-354 (抗結核)

5mg

SC3319-25mg

TBA-354 (抗結核)

25mg

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說明書

1份