Size | Price | Stock | Qty |
---|---|---|---|
500mg |
|
||
Other Sizes |
|
Targets |
Dihydrofolate reductase, Bacteria[1] Influenza A virus[4]
|
---|---|
ln Vitro |
Dihydrofolase reductase (DHFR), which converts dihydrofolate to tetrahydrofolate (THF), is inhibited by trimethoprim, which stops the metabolism of folate[1]. Heat shock proteins (Hsps) and protein aggregation are induced in E. coli by trimethoprim (3 μg/mL; 1 h). coli cells, suggesting that protein misfolding is caused by the presence of trimethoprim sulfate[1]. DnaK, DnaJ, GroEL, ClpB, and IbpA/B Hsps are all inducible in E when treated with trimethoprim (1.5–3 μg/mL; 1 h). Coli cells subjected to heat stress and folate[1].
|
ln Vivo |
Trimethoprim (10 mg/kg; iv; once every 12 h; 3 d) demonstrates antibacterial action in infected mice against H. influenzae, S. pneumoniae, E. coli, and N. meningitidis[2]. Trimethoprim has a MIC value of approximately 1 μM against E. coli and can be linked to thiomaltose (TM-TMP). It also exhibits stability with a half-life of approximately 1 hour in full serum[2]. Trimethoprim (10 mg/mL; 0.5 mL; inject with Trimethoprim-Zn mixed suspension) raises the survival rate of chicken embryos while lowering the viral titer[4].
|
Animal Protocol |
Animal/Disease Models: Female C3H/HeOuJ mice (transurethrally infected with a 50 μL suspension containing 1-2×107 CFU of E. coli under 3% isoflurane)[2]
Doses: 10 mg/kg Route of Administration: iv; once every 12 h; for 3 d Experimental Results: demonstrated 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/Disease Models: Fertilized eggs (injected H3N2 virus into amniotic and allantoic space at day 8)[4] Doses: 10 mg/mL; 0.5 mL Route of Administration: The Trimethoprim-Zn combined suspension was injected into the air sac; single dosage Experimental Results: diminished the virus titer and increased the survival rate of chicken embryo. The survival rate peaked at ratio about 0.18 (Zn/Trimethoprim). |
References |
[1]. Ewa Laskowska, et al. Trimethoprim Induces Heat Shock Proteins and Protein Aggregation in E. Coli Cells. Curr Microbiol. 2003 Oct;47(4):286-9.
[2]. R N Brogden, et al. Trimethoprim: A Review of Its Antibacterial Activity, Pharmacokinetics and Therapeutic Use in Urinary Tract Infections. Drugs. 1982 Jun;23(6):405-30. [3]. Xiaojian Wang, et al. A Trimethoprim Conjugate of Thiomaltose Has Enhanced Antibacterial Efficacy In Vivo. Bioconjug Chem. 2018 May 16;29(5):1729-1735. [4]. El Habbal MH. Combination therapy of zinc and trimethoprim inhibits infection of influenza A virus in chick embryo. Virol J. 2021 Jun 3;18(1):113. |
Molecular Formula |
C17H24N4O6
|
---|---|
Molecular Weight |
380.40
|
CAS # |
23256-42-0
|
Related CAS # |
Trimethoprim;738-70-5;Trimethoprim-d3;1189923-38-3;Trimethoprim sulfate;56585-33-2;Trimethoprim hydrochloride;60834-30-2;Trimethoprim-13C3;1189970-95-3
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
O(C([H])([H])[H])C1C(=C(C([H])=C(C=1[H])C([H])([H])C1=C([H])N=C(N([H])[H])N=C1N([H])[H])OC([H])([H])[H])OC([H])([H])[H].O([H])C([H])(C(=O)O[H])C([H])([H])[H]
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : 250 mg/mL (657.20 mM)
H2O : 16.67 mg/mL (43.82 mM) |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2 mg/mL (5.26 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6288 mL | 13.1441 mL | 26.2881 mL | |
5 mM | 0.5258 mL | 2.6288 mL | 5.2576 mL | |
10 mM | 0.2629 mL | 1.3144 mL | 2.6288 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.