Trimethoprim

738-70-5

290.32

DMSO : 50 mg/mL (172.22 mM; Need ultrasonic); H2O : 0.67 mg/mL (2.31 mM; Need ultrasonic)

Cell Cycle/DNA Damage; Anti-infection; Anti-infection

Trimethoprim is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim has the potential for urinary tract infections, Shigellosis and Pneumocystis pneumonia treatment^[1][2][3]. IC50 & Target: Dihydrofolate reductase^[1]
Bacteria^[1] In Vitro: Trimethoprim interrupts folate metabolism by inhibition of the activity of dihydrofolase reductase (DHFR), which reduces dihydrofolate to tetrahydrofolate (THF)^[1].
Trimethoprim causes protein aggregation and induction of main heat shock proteins (Hsps) in E. coli cells, which indicates that Trimethoprim presence leads to protein misfolding. Trimethoprim causes induction of DnaK, DnaJ, GroEL, ClpB, and IbpA/B Hsps. Among these Hsps, IbpA/B are most efficiently induced by Trimethoprim and coaggregates with the insoluble proteins. Upon folate stress, deletion of the delta ibpA/B operon resulted in increased protein aggregation but does not influence cell viability^[1]. In Vivo: In intraperitoneal infections in mice, the CD₅₀ values for Trimethoprim alone against H. influenzae, S. pneumoniae, E. coli and N. meningitidis, is 150 mg/kg, 335 mg/kg, 27.5 mg/kg and 8.4 mg/kg, respectively^[2].