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TBA354
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
TBA354图片
CAS NO:1257426-19-9
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)询价
5mg询价
25mg询价

TBA354 是一种有效的抗结核化合物；保持对结核分枝杆菌 H37Rv 同基因单耐药菌株的活性。
Cas No.1257426-19-9
化学名(S)-2-nitro-6-((6-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)methoxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine
Canonical SMILESFC(F)(OC1=CC=C(C2=NC=C(CO[C@@]3([H])CN4C=C(N(=O)=O)N=C4OC3)C=C2)C=C1)F
分子式C19H15F3N4O5
分子量436.34
溶解度≥ 17.6mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

TBA354 is a new antitubercular agent [1].

TBA354 is a pyridine-containing biaryl compound against Mycobacterium tuberculosis. In 10 M. tuberculosis strains tested, the MIC range for TBA-354 was<0.02 to 0.36 μM. The MICs against S.aureus, E. coli, and C. albicans were >50 μM, suggesting TBA-354 is a narrow-spectrum agent. In Caco-2 cell bidirectional permeability assay, TBA-354 showed high permeability at 1 and 10 μM. TBA-354 was metabolically stable or moderately metabolized in incubations with liver microsomes. In HLM, TBA-354 (30 μM) showed weak inhibition of CYP3A4-catalyzed testosterone 6-hydroxylation by 40% [1].

In a low-dose aerosol infection model, TBA-354 dosed with 100 mg/kg daily for 5 of 7 days per week for 3 weeks showed significant bactericidal activity and reduced lung CFU by approximately 1 log10. In chronic murine TB, TBA-354 killed M. tuberculosis in a dose- and time-dependent way, and exhibited significant bactericidal activity. TBA-354 has high bioavailability and a long elimination half-life [1]. In murine models of tuberculosis, TBA-354 significantly increased the sterilizing activity of bedaquiline [2].

References:
[1].  Upton AM, Cho S, Yang TJ, et al. In vitro and in vivo activities of the nitroimidazole TBA-354 against Mycobacterium tuberculosis. Antimicrob Agents Chemother, 2015, 59(1): 136-144.
[2].  Tasneen R, Williams K, Amoabeng O, 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, 59 :129-135.

 
 
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