Trimethoprim hydrochloride 是一种抑菌抗生素 (antibiotic)，也是一种具有口服活性的二氢叶酸还原酶 (dihydrofolate reductase) 抑制剂。Trimethoprim hydrochloride 对多种革兰氏阳性 (Gram-positive) 和革兰氏阴性需氧细菌 (Gram-negative aerobic bacteria) 具有活性。Trimethoprim hydrochloride 可用于尿路感染，志贺氏菌病和肺孢子菌肺炎的研究。Trimethoprim hydrochloride 与锌联合使用可抑制甲型流感病毒 (Influenza A virus) 对鸡胚的感染。
| 生物活性 | Trimethoprim hydrochloride is a bacteriostaticantibioticand an orally activedihydrofolate reductaseinhibitor. Trimethoprim hydrochloride is active against a wide range ofGram-positiveandGram-negative aerobic bacteria. Trimethoprim hydrochloride has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim hydrochloride can inhibitinfectionofInfluenza A virusin chick embryo when combinated with zinc[1][2][3][4]. |
| IC50& Target | Dihydrofolate reductase, Bacteria[1]
Influenza A virus[4] |
体外研究
(In Vitro) | Trimethoprim interrupts folate metabolism by inhibition of the activity of dihydrofolase reductase (DHFR), which reduces dihydrofolate to tetrahydrofolate (THF)[1].
Trimethoprim (3 μg/mL; 1 h) induces protein aggregation and main heat shock proteins (Hsps) in E. coli cells, which indicates that Trimethoprim sulfate presence leads to protein misfolding[1].
Trimethoprim (1.5-3 μg/mL; 1 h) causes induction of DnaK, DnaJ, GroEL, ClpB, and IbpA/B Hsps inE. colicells exposed to folate and heat stress[1].
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体内研究
(In Vivo) | Trimethoprim (10 mg/kg; i.v.; once every 12 h; 3 d) shows antibacterial activity againstH. influenzae,S. pneumoniae,E. coliandN. meningitidisin infected mice[2].
Trimethoprim can be connected with the thiomaltose (TM-TMP) and shows stability with a half-life of about 1 hour in complete serum, and has an MIC value around 1 μM againstE. coli[2].
Trimethoprim (10 mg/mL; 0.5 mL; inject with Trimethoprim-Zn combined suspension) decreases the virus titer and increases the survival rate of chicken embryo[4].
| Animal Model: | Female C3H/HeOuJ mice (transurethrally infected with a 50 μL suspension containing 1-2×107CFU ofE. coliunder 3% isoflurane)[2] | | Dosage: | 10 mg/kg | | Administration: | i.v.; once every 12 h; for 3 d | | Result: | Showed antibacterial activity againstH. influenzae,S. pneumoniae,E. coliandN. meningitidiswith 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)[4] | | 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). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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