中文同义词:
乳酸甲氧苄啶 1G;2,4-二氨基-5-(3,4,5-三甲氧基苄基)嘧啶乳酸盐;甲氧苄啶 乳酸盐;乳酸三甲氧苄氨嘧啶;甲氧苄氨嘧啶乳酸盐;乳酸甲氧苄啶;乳酸甲氧苄氨嘧啶;TRIMETHOPRIM LACTATE SALT 乳酸甲氧苄啶
英文名称:
Trimethoprim lactate salt
英文同义词:
lactic acid, compound with 5-(3,4,5-trimethoxybenzyl)pyrimidine-2,4-diamine (1:1);5-(3,4,5-triMethoxybenzyl)pyriMidine-2,4-diaMine 2-hydroxypropanoate;Lactic triMethopriM;Trimethoprim lactate, >=99%;5-(3,4,5-Trimethoxybenzyl);pyrimidine-2,4-diamine 2-hydroxypropanoate;2,4-DIAMINO-5-(3,4,5-TRIMETHOXYBENZYL)PYRIMIDINE LACTATE;2,4-diamino-5-(3,4,5-trimethoxybenzyl)pyrimidine lactate salt
相关类别:
化合物：原料药;生化试剂;抗生素;中间体 Intermediate;兽药;饲料添加剂;医药原料药;兽药原料;医药原料;抗生素类;医药化工类;化学试剂;中间体;原料中间体-原料药;原料药;原料药;农用兽用原料;医用原料;医药、农药及染料中间体;陕西林奈主打产品
储存条件
Keep in dark place,Inert atmosphere,2-8°C
CAS 数据库
23256-42-0(CAS DataBase Reference)
生物活性
Trimethoprim lactic 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 lactic 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 lactic 可用于尿路感染，志贺氏菌病和肺孢子菌肺炎的研究。
靶点
Dihydrofolate reductase
Bacteria
体外研究
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.
体内研究
In intraperitoneal infections in mice, the CD 50 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.
