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Catalog No.
Folate antagonist,inhibits DFHR
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
In stock
In stock
In stock
In stock

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Methotrexate, a folate antagonist, is a potent anti-inflammatory agent when used weekly in low concentrations, the anti-phlogistic action of which is due to increased adenosine release at inflamed sites. Studies have demonstrated that methotrexate polyglutamates are active inhibitors of several enzymatic reactions, including dihydrofolate reductase. On consideration of biochemical pharmacology of methotrexate of methotrexate, it is taken up by cells and tissues and converted to methotrexate–polyglutamates, long-lived derivatives that retain biochemical and biologic activity within the cell. There is evidence that methotrexate does not act in rheumatoid arthritis (RA) simply as a cytotoxic agent for the cells responsible for the inflammation.


Bruce N. Cronstein, Dwight Naime, Edward Ostad. The antiinflammatory mechanism of methotrexate. Increased adenosine release at inflamed sites diminishes leukocyte accumulation in an in vivo model of inflammation. Journal of Clinical Investigation. 1993 December; 92(6): 2675–2682.

Bruce N. Cronstein. The mechanism of action of methotrexate. Rheumatic Disease Clinics of North America Volume 23, Issue 4, 1 November 1997, Pages 739–755.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.59-05-2
SynonymsAmethopterin, Rheumatrex, Abitrexate, Methylaminopterin, Antifolan, Trexall, Ledertrexate
Solubility≥21.55 mg/mL in DMSO,insoluble in EtOH,insoluble in H2O
Chemical Name(2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanedioic acid
SDFDownload SDF
Canonical SMILESCN(CC1=CN=C2C(=N1)C(=NC(=N2)N)N)C3=CC=C(C=C3)C(=O)NC(CCC(=O)O)C(=O)O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.


Cell experiment [1]:

Cell lines

activated T cells from human peripheral blood

Preparation method

The solubility of this compound in DMSO is >21.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.1-10 μM, 1-24 h


Methotrexate (0.1-10 μM) induced apoptosis of activated T cells from human peripheral blood. In PBL, treatment with MTX for 8 h induced apoptosis. Methotrexate at low (0.01 μM) and high (100 μM) concentrations inhibited cell proliferation without inducing apoptosis. Methotrexate-induced apoptosis required progression to the S phase of the cell cycle.

Animal experiment [2,3]:

Animal models


Dosage form

Intraperitoneal injection, 2 mg/kg, once daily


MTX exposure reduced thymus and spleen indices of mice. Methotrexate (≥5 mg/kg) markedly decreased white blood cells, thymic and splenic lymphocytes. Intraperitoneal injection with methotrexate for 3-4 wk increased splenocyte AICAR content, raised adenosine concentrations in exudates from carrageenan-inflamed air pouches, and markedly inhibited leukocyte accumulation in inflamed air pouches in mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.


[1]. Genestier L, Paillot R, Fournel S, et al. Immunosuppressive properties of methotrexate: apoptosis and clonal deletion of activated peripheral T cells[J]. Journal of Clinical Investigation, 1998, 102(2): 322.

[2]. Gu S, Wu Y, Yang J. Screening of cytoprotectors against methotrexate-induced cytogenotoxicity from bioactive phytochemicals[J]. PeerJ, 2016, 4: e1983.

[3]. Cronstein B N, Naime D, Ostad E. The antiinflammatory mechanism of methotrexate. Increased adenosine release at inflamed sites diminishes leukocyte accumulation in an in vivo model of inflammation[J]. Journal of Clinical Investigation, 1993, 92(6): 2675.

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