Trimethoprim 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 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 可用于尿路感染，志贺氏菌病和肺孢子菌肺炎的研究。Trimethoprim 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 is a bacteriostaticantibioticand an orally activedihydrofolate reductaseinhibitor. Trimethoprim is active against a wide range ofGram-positiveandGram-negative aerobic bacteria. Trimethoprim has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim 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 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(172.22 mM;Need ultrasonic) H2O : 0.67 mg/mL(2.31 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.4445 mL | 17.2224 mL | 34.4447 mL | | 5 mM | 0.6889 mL | 3.4445 mL | 6.8889 mL | | 10 mM | 0.3444 mL | 1.7222 mL | 3.4445 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (8.61 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.61 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (8.61 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.61 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.61 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.61 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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