Methotrexate
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
氨甲蝶呤是一种叶酸拮抗剂，低浓度下每周使用具有强效的抗炎作用，这种抗炎作用是由于炎症部位腺苷释放增加。研究表明，氨甲蝶呤多聚谷氨酸是包括二氢叶酸还原酶在内的几个酶促反应的抑制剂。氨甲蝶呤由细胞和组织吸收，并转换为氨甲蝶呤多聚谷氨酸，这种衍生物长时间在细胞内保留生物化学活性。有证据表明，在类风湿性关节炎（RA）中，氨甲蝶呤作为细胞毒性剂对炎症的细胞发挥作用。
参考文献：
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.
- 1.Goodspeed A, Jean A, et al. "A Whole-genome CRISPR Screen Identifies a Role of MSH2 in Cisplatin-mediated Cell Death in Muscle-invasive Bladder Cancer." Eur Urol. 2019 Feb;75(2):242-250. PMID:30414698
- 2.Andrew Goodspeed, Annie Jean, et al. "Low MSH2 protein levels identify muscle-invasive bladder cancer resistant to cisplatin." bioRxiv. 2018 June 29
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 454.44 |
| Cas No. | 59-05-2 |
| Formula | C20H22N8O5 |
| Synonyms | Amethopterin, 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 |
| SDF | Download SDF |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
来自人外周血的活化T细胞 |
|
溶解方法 |
该化合物在DMSO中的溶解度大于21.6 mg/mL。若获取更高浓度的溶液，可在37℃下孵育10分钟，随后在超声波浴中摇匀。-20℃以下可储存数月。 |
|
反应条件 |
0.1-10 μM，1-24 h |
|
应用 |
Methotrexate（0.1-10 μM）诱导来自人外周血的活化T细胞的凋亡。在PBL中，MTX处理8小时诱导细胞凋亡。Methotrexate在低（0.01 μM）和高（100 μM）浓度下抑制细胞增殖而不诱导细胞凋亡。Methotrexate诱导的凋亡需要进展到细胞周期的S期。 |
| 动物实验 [2,3]: | |
|
动物模型 |
小鼠 |
|
给药剂量 |
腹腔注射，2 mg/kg，每日一次 |
|
应用 |
Methotrexate暴露降低小鼠胸腺和脾脏指数。Methotrexate(≥5 mg/kg)明显降低白细胞、胸腺和脾淋巴细胞。腹腔注射methotrexate 3-4周可增加脾细胞AICAR含量，提高角叉菜胶发炎空气囊渗出液中的腺苷浓度，并显著抑制小鼠发炎空气囊中的白细胞积聚。 |
|
注意事项 |
由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。 |
|
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. |
|
质量控制和MSDS
- 批次:
化学结构
相关生物数据
