CAS NO: | 1257426-19-9 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
25mg | 电议 |
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 SMILES | FC(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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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: |