TBA354 有抗结核作用,对结核分枝杆菌H37Rv菌株具有活性。
产品描述
TBA-354 is a potent anti-tuberculosis compound.
体外活性
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 [1]. 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 [2].
体内活性
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.
Cas No.
1257426-19-9
分子式
C19H15F3N4O5
分子量
436.347
别名
TBA 354
储存和溶解度
DMSO:46 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years