产品
编 号:F443858
分子式:C14H18N4O3
分子量:290.32
产品类型
结构图
CAS No: 738-70-5
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产品详情
生物活性:
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 the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim can inhibit infection of Influenza A virus in chick embryo when combinated with zinc.
体内研究:
Trimethoprim (10 mg/kg;静脉注射;每 12 小时一次;3 天) 显示出对 H 的抗菌活性。流感病菌,肺炎链球菌,大肠杆菌和脑膜炎球菌感染小鼠的保护作用。Trimethoprim 可与硫麦芽糖 (TM-TMP) 结合并表现出稳定性,在完全血清中的半衰期约为 1 小时,并且对大肠杆菌的 MIC 值约为 1 μM。Trimethoprim (10 mg/mL;0.5 mL;甲氧苄氨嘧啶-锌复悬液注射) 降低病毒滴度,提高鸡胚存活率。Animal Model:Female C3H/HeOuJ mice (transurethrally infected with a 50 μL suspension containing 1-2×107 CFU of E. coli under 3% isoflurane)
Dosage:10 mg/kg
Administration:i.v.; once every 12 h; for 3 d
Result:Showed antibacterial activity against H. influenzae, S. pneumoniae, E. coli and N. meningitidis with CD50s of 150 mg/kg, 335 mg/kg, 27.5 mg/kg and 8.4 mg/kg, respectively in infected mice.
Animal Model:Fertilized eggs (injected H3N2 virus into amniotic and allantoic space at day 8)
Dosage:10 mg/mL; 0.5 mL
Administration:The Trimethoprim-Zn combined suspension was injected into the air sac; single dosage
Result:Decreased the virus titer and increased the survival rate of chicken embryo.The survival rate peaked at ratio about 0.18 (Zn/Trimethoprim).
体外研究:
Trimethoprim 通过抑制二氢叶酸还原酶 (DHFR) 的活性来中断叶酸代谢,该酶将二氢叶酸还原为四氢叶酸 (THF)。Trimethoprim (3 μg/mL;1 小时) 诱导大肠杆菌细胞中的蛋白质聚集和主要热休克蛋白 (Hsps),这表明硫酸 Trimethoprim 的存在导致蛋白质错误折叠。Trimethoprim (1.5-3 μg/mL;1 h) 诱导大肠杆菌的 DnaK、DnaJ、GroEL、ClpB 和 IbpA/B Hsps,而诱导细胞暴露于叶酸和热应激。