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Trimethoprim

CAS No. : 738-70-5

MCE 站：Trimethoprim

产品活性：Trimethoprim 是一种抑菌抗生素，也是一种具有口服活性的二氢叶酸还原酶 (dihydrofolate reductase) 抑制剂。Trimethoprim 对多种革兰氏阳性和革兰氏阴性需氧细菌 (Gram-positive 和 Gram-negative aerobic bacteria) 具有活性。Trimethoprim 可用于尿路感染，志贺氏菌病和肺孢子菌肺炎的研究。

研究领域：Cell Cycle/DNA Damage  |  Anti-infection

作用靶点：Antifolate  |  Bacterial  |  Antibiotic

In Vitro: Trimethoprim interrupts folate metabolism by inhibition of the activity of dihydrofolase reductase (DHFR), which reduces dihydrofolate to tetrahydrofolate (THF).
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.

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.

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