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MethotrexateFolate antagonist,inhibits DFHR

Methotrexate

Catalog No. A4347
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
100mg $50.00 In stock
200mg $80.00 In stock
500mg $130.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

Methotrexate

Protocol

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

Applications

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

Mice

Dosage form

Intraperitoneal injection, 2 mg/kg, once daily

Application

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.

References:

[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.

Methotrexate Dilution Calculator

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Chemical Properties

Cas No. 59-05-2 SDF Download SDF
Synonyms Amethopterin, Rheumatrex, Abitrexate, Methylaminopterin, Antifolan, Trexall, Ledertrexate
Chemical Name (2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanedioic acid
Canonical SMILES CN(CC1=CN=C2C(=N1)C(=NC(=N2)N)N)C3=CC=C(C=C3)C(=O)NC(CCC(=O)O)C(=O)O
Formula C20H22N8O5 M.Wt 454.44
Solubility >21.6mg/mL in DMSO Storage Store at -20°C
General tips For 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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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.

Reference

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.