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。
货号:ajcx36368
CAS:864941-32-2
分子式:C16H13N3O4S2
分子量：375.42
溶解度:DMSO : 125 mg/mL (332.96 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

TCA1 is a small molecule with activity against drug-susceptible and -resistant Mycobacterium tuberculosis (Mtb). TCA1 inhibits enzymes involved in cell wall and molybdenum cofactor biosynthesis, such as DprE1 and MoeW[1].

TCA1 shows bactericidal activity against both replicating (WT and drug resistant) and nonreplicating Mycobacterium tuberculosis (Mtb). TCA1 inhibits biofilm formation by Mtb H37Rv[1]. 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[1].

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[1].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[1].BALB/c mice infected with Mtb H37Rv[1]40 mg/kgOral gavage; 1 time/d for 5 d/week; for 4 weeksEffectively inhibits Mtb in vivo.

[1]. Feng Wang, et al. Identification of a small molecule with activity against drug-resistant and persistent tuberculosis. Proc Natl Acad Sci U S A. 2013 Jul 2;110(27):E2510-7.