Methotrexate
(Synonyms: 甲氨蝶呤; Amethopterin; CL14377; WR19039) 目录号 : GC10405
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。
Cas No.:59-05-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
activated T cells from human peripheral blood |
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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. |
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Reacting condition |
0.1-10 μM, 1-24 h |
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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]: | |
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Animal models |
Mice |
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Dosage form |
Intraperitoneal injection, 2 mg/kg, once daily |
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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. |
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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. |
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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. |
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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.
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.
| Cas No. | 59-05-2 | SDF | |
| 别名 | 甲氨蝶呤; Amethopterin; CL14377; WR19039 | ||
| 化学名 | (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 | ||
| 分子式 | C20H22N8O5 | 分子量 | 454.44 |
| 溶解度 | ≥ 21.55 mg/mL in DMSO | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2005 mL | 11.0026 mL | 22.0051 mL |
| 5 mM | 0.4401 mL | 2.2005 mL | 4.401 mL |
| 10 mM | 0.2201 mL | 1.1003 mL | 2.2005 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。