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TCA1

CAS No. : 864941-32-2

MCE 站：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。

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 C_max (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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