| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Mouse macrophage swelling caused by Toxoplasma gondii is entirely inhibited by trimetrexate (0.1 μM, 18 h) [3]. Toxoplasma gondii cell membranes are permeable to trimetrexate (1 μM), which quickly reaches high intracellular concentrations (108 pmol/107 cells). In SNU-C4 and NCI-H630 cell lines, trimetrexate (0.1 mM; 24 hours) reduces cell growth by 50–60% [5]. For ten minutes, trimetrexate (1 and 10 mM; 24 hours) in C4 was added [3].
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| ln Vivo |
Trimetrexate (180 mg/kg or 30 mg/kg; po or intraperitoneal injection; daily) prolongs the median survival of Toxoplasma gondii infection and shows anti-Toxoplasma activity [3]. Trimetrexate (0-30 mg/kg; iv; once daily for 5 days) exhibits chronic toxicity in toxicity [4].
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| Cell Assay |
Cell Proliferation Assay[5]
Cell Types: SNU-C4 and NCI-H630 Tested Concentrations: 0.1 mM Incubation Duration: 24 h Experimental Results: Both cell lines inhibited cell growth by 50-60%. Cell proliferation assay[5] Cell Types: C4 Cell Tested Concentrations: 1 and 10 mM Incubation Duration: 24 hrs (hours) Experimental Results: Produced 42% and 50% lethality at 1 and 10 mM respectively. |
| Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse infected with Toxoplasma gondii, weighing about 20 g [3]
Doses: 180 mg/kg or 30 mg/kg Dosing: 180 mg/kg orally daily in drinking water or intraperitoneal (ip) injection 30 times daily mg/kg Experimental Results: Extended median survival of infected mice to 10 days (oral) or 19 days (ip). Animal/Disease Models: Charles River Wistar Crl(WI)BR rats, weighing approximately 150 to 200 g[4] Doses: 0, 1, 10 or 30 mg/kg Route of Administration: intravenous (iv) (iv)injection, one time/day for 5 days, then 23- Experimental Results: Showing chronic toxicity, testicular changes that persisted over the course of multiple dosing cycles were irreversible within 21 days but required an additional 56 days for essentially complete recovery. |
| References |
[1]. Hopper AT, et al. Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis. J Med Chem. 2019 Feb 14;62(3):1562-1576.
[2]. Fulton, B., et al. Trimetrexate. Drugs 49, 563–576 (1995). [3]. Allegra CJ, et al. Potent in vitro and in vivo antitoxoplasma activity of the lipid-soluble antifolate trimetrexate. J Clin Invest. 1987 Feb;79(2):478-82. [4]. Dethloff LA, et al. Chronic toxicity of the anticancer agent trimetrexate in rats. Fundam Appl Toxicol. 1992 Jul;19(1):6-14. [5]. Grem JL, Voeller DM, Geoffroy F, Horak E, Johnston PG, Allegra CJ. Determinants of trimetrexate lethality in human colon cancer cells. Br J Cancer. 1994 Dec;70(6):1075-84. |
| Molecular Formula |
C19H23N5O3
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|---|---|
| Molecular Weight |
369.41762
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| CAS # |
52128-35-5
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| Related CAS # |
Trimetrexate glucuronate;82952-64-5;Trimetrexate trihydrochloride;1658520-97-8;Trimetrexate isethionate;82935-04-4
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
NC1=C(C(C)=C2CNC3=CC(OC)=C(OC)C(OC)=C3)C(C=C2)=NC(N)=N1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 61.5 mg/mL (~166.48 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.77 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 25.0 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: ≥ 2.5 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 40 mg/mL (108.28 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7069 mL | 13.5347 mL | 27.0695 mL | |
| 5 mM | 0.5414 mL | 2.7069 mL | 5.4139 mL | |
| 10 mM | 0.2707 mL | 1.3535 mL | 2.7069 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.
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