耗材描述
TCA1
产品活性:TCA1 是一种小分子,具有抗耐药性和敏感性结核分枝杆菌 (Mtb) 的活性。TCA1 抑制参与细胞壁和钼辅因子生物合成的酶,如 DprE1 和 MoeW。
产品来源: https://www.medchemexpress.cn/tca1.html
研究领域:Anti-infection
作用靶点:Bacterial
In Vitro: TCA1 shows bactericidal activity against both replicating (WT and drug resistant) and nonreplicating Mycobacterium tuberculosis (Mtb). TCA1 inhibits biofilm formation by Mtb H37Rv.
TCA1 shows selective inhibitory activity against bacterial growth-it is inactive against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa, suggesting that the target for its bactericidal activity is specific to the genus Mycobacterium.
In Vivo: TCA1 (40 mg/kg; oral gavage; 1 time/d for 5 d/week; for 4 weeks) is efficacious in acute and chronic Mtb infection mouse models.
In a mouse model of Mtb infection, after i.v. administration, TCA1 exhibits a low clearance and steady-state volume of distribution, with an elimination half-life of 0.73 h. After oral administration of 20 and 50 mg/kg in solution formulation, TCA1 shows a high Cmax (2122 and 5653 nM, respectively), moderate exposure with oral bioavailability ranging from 19% to 46%, and a half-life of 1.8 h.
BALB/c mice infected with Mtb H37Rv
40 mg/kg
Oral gavage; 1 time/d for 5 d/week; for 4 weeks
Effectively inhibits Mtb in vivo.
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