产品描述: | TBA-354 is a potent anti-tuberculosis compound. |
靶点: |
Antibiotic;Antibacterial;Antibacterial; Antibiotic |
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 Clinicalal 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. |
参考文献: |
1. Tasneen R, et al. Contribution of the nitroimidazoles PA-824 and TBA-354 to the activity of novel regimens in murine models of tuberculosis. Antimicrob Agents Chemother. 2015 Jan;59(1):129-35. 2. Upton AM, et al. In vitro and in vivo activities of the nitroimidazole TBA-354 against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2015 Jan;59(1):136-44. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.292 ml |
11.459 ml |
22.918 ml |
5 mM |
0.458 ml |
2.292 ml |
4.584 ml |
10 mM |
0.229 ml |
1.146 ml |
2.292 ml |
50 mM |
0.046 ml |
0.229 ml |
0.458 ml |
|
注意: |
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