Methotrexate

甲氨蝶呤 (Amethopterin) 是一种抗代谢物和抗叶酸剂，可抑制二氢叶酸还原酶，从而阻止叶酸转化为四氢叶酸，并抑制 DNA 合成。

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100mg

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200mg

￥700.00

560.00

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货号: ajci5052
CAS: 59-05-2
别名: 甲氨蝶呤; Amethopterin; CL14377; WR19039
分子式: C20H22N8O5
分子量: 454.44
纯度: ＞98%
溶解度: ≥ 21.55 mg/mL in DMSO
储存: -20°C
库存: 现货

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.

甲氨蝶呤是一种叶酸拮抗剂，在低浓度下每周使用时是一种强效的抗炎药物，其抗炎作用是由于在发炎部位增加了腺苷释放。研究表明，甲氨蝶呤多聚谷氨酸是多种酶反应的有效抑制剂，包括二氢叶酸还原酶。在考虑甲氨蝶呤的生物化学药理学时，它被细胞和组织吸收并转化为甲氨蝶呤多聚谷氨酸，这是一种长寿命的衍生物，在细胞内保留生物化学和生物活性。有证据表明，甲氨蝶呤在类风湿性关节炎（RA）中的作用并不仅仅是细胞毒性剂，作用于负责炎症的细胞。

Reference

[1].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.
[2].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.

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.
参考文献: [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.