PeptideDB

TCA1

CAS: 864941-32-2 F: C16H13N3O4S2 W: 375.42

TCA1 is a small molecule with activity against drug-susceptible and -resistant Mycobacterium tuberculosis (Mtb). TCA1 in
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Bioactivity 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].
Invitro 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].
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[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.
Name TCA1
CAS 864941-32-2
Formula C16H13N3O4S2
Molar Mass 375.42
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Reference [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.