Methotrexate (hydrate)
(Synonyms: 二水合氨甲嘌呤) 目录号 : GC47649
A folic acid and aminopterin derivative
Cas No.:133073-73-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Methotrexate (MTX) is similar in structure to folic acid and aminopterin . It acts by inhibiting the metabolism of folic acid and blocking key enzymes in the synthesis of purines and pyrimidines required for cell proliferation.1,2 MTX is known to induce adenosine release, which mediates many of its anti-inflammatory effects, including the reduction of proinflammatory cytokines.2,3,4 Formulations containing MTX have been used in the treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions.5,6 MTX formulations have been considered the gold standard of disease-modifying antirheumatic drug (DMARD) therapy to treat both the immune-inflammatory and joint destructive processes of rheumatoid arthritis.7
1.Tian, H., and Cronstein, B.N.Understanding the mechanisms of action of methotrexate: Implications for the treatment of rheumatoid arthritisBull. NYU Hosp. Jt. Dis.65(3)168-173(2007) 2.Swierkot, J., and Szechinski, J.Methotrexate in rheumatoid arthritisPharmacol. Rep.58(4)473-492(2006) 3.Chan, E.S.L., and Cronstein, B.N.Molecular action of methotrexate in inflammatory diseasesArthritis Res.4(4)266-273(2002) 4.Wessels, J.A.M., Huizinga, T.W.J., and Guchelaar, H.J.Recent insights in the pharmacological actions of methotrexate in the treatment of rheumatoid arthritisRheumatology47249-255(2008) 5.Cutolo, M., Sulli, A., Pizzorni, C., et al.Anti-inflammatory mechanisms of methotrexate in rheumatoid arthritisAnn. Rheum. Dis.60(8)729-735(2001) 6.Christin-Maitre, S., Bouchard, P., and Spitz, I.M.Medical termination of pregnancyN. Engl. J. Med.342(13)946-956(2000) 7.Smolen, J.S., and Steiner, G.Therapeutic strategies for rheumatoid arthritisNat. Rev. Drug Dis.2(6)473-488(2003)
| Cas No. | 133073-73-1 | SDF | |
| 别名 | 二水合氨甲嘌呤 | ||
| Canonical SMILES | NC1=NC(N)=C2C(N=CC(CN(C3=CC=C(C(N[C@H](C(O)=O)CCC(O)=O)=O)C=C3)C)=N2)=N1.O | ||
| 分子式 | C20H22N8O5.XH2O | 分子量 | 454.4 |
| 溶解度 | DMF: 14 mg/ml,DMSO: 3 mg/ml,PBS (pH 7.2): 1 mg/ml | 储存条件 | Store at -20°C |
| 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 | 2.2007 mL | 11.0035 mL | 22.007 mL |
| 5 mM | 0.4401 mL | 2.2007 mL | 4.4014 mL |
| 10 mM | 0.2201 mL | 1.1004 mL | 2.2007 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。
Methotrexate: new therapeutic approaches
Actas Dermosifiliogr 2014 Jul-Aug;105(6):583-9.PMID:23434058DOI:10.1016/j.ad.2012.11.017.
Although the first study on the efficacy of Methotrexate in the treatment of psoriasis was reported in 1958, scientific evidence for this indication has been scant until quite recently. We now have new data on the pharmacokinetics and mechanism of action of Methotrexate and new subcutaneous formulations that have improved the bioavailability, efficacy, and ease of administration of the drug. The results of recent clinical trials comparing Methotrexate with several biologic agents have shown it to be the first-line therapy among the classic systemic treatments for psoriasis. Moreover, the incremental cost-effectiveness ratio for subcutaneous Methotrexate has been shown to be superior to that of ciclosporin, adalimumab, and infliximab.
Side effects of Methotrexate therapy for rheumatoid arthritis: A systematic review
Eur J Med Chem 2018 Oct 5;158:502-516.PMID:30243154DOI:10.1016/j.ejmech.2018.09.027.
Methotrexate (MTX) is used as an anchor disease-modifying anti-rheumatic drugs (DMARDs) in treating rheumatoid arthritis (RA) because of its potent efficacy and tolerability. MTX benefits a large number of RA patients but partially suffered from side effects. A variety of side effects can be associated with MTX when treating RA patients, from mild to severe or discontinuation of the treatment. In this report, we reviewed the possible side effects that MTX might cause from the most common gastrointestinal toxicity effects to less frequent malignant diseases. In order to achieve regimen with less side effects, the administration of MTX with appropriate dose and a careful pretreatment inspection is necessary. Further investigations are required when combining MTX with other drugs so as to enhance the efficacy and reduce side effects at the same time. The management of MTX treatment is also discussed to provide strategies for occurred side effects. Thus, this review will provide scholars with a comprehensive understanding the side effects of MTX administration by RA patients.
Methotrexate therapy
Can J Gastroenterol 1998 Jan-Feb;12(1):26-7.PMID:9544409doi
Methotrexate may be very helpful for your illness if proper care is taken in the use of this medication. Follow your physician's instructions faithfully. Take Methotrexate weekly as directed. Notify your physician at once if an accidental overdose is suspected or if you develop fever, cough or shortness of breath. If you develop vomiting, there is a change in your pattern of diarrhea or you suspect that you are dehydrated, notify your physician before taking the next dose of Methotrexate. Do not start or change any medicine without first checking with your physician. Avoid or severely restrict alcohol, including wine and beer. Obtain the blood tests ordered by your physician. Avoid pregnancy during and for several months after taking Methotrexate. Keep Methotrexate out of the reach of children. It has been prescribed for your current medical problem and must not be given to other people.
Intrathecal methotrexate-induced neurotoxicities
Am J Hosp Pharm 1981 Jan;38(1):65-8.PMID:7011005doi
The pharmacokinetics, therapeutic index, neurotoxicities, methods of administration, and dosages of intrathecal Methotrexate are reviewed. The intrathecal administration of Methotrexate can provide therapeutic concentrations in the cerebrospinal fluid (CSF) without the use of high-dose intravenous Methotrexate. Major neurologic complications have been reported to occur in 3--40% of patients following intrathecal Methotrexate. The development of neurotoxicity is related to dose, concentration of Methotrexate in the CSF, age of the patient, anatomical and physiological abnormalities in the CNS, type of dilutional vehicle, intracranial radiation, and intravenous Methotrexate. Substantial evidence is lacking that chemical preservatives and Methotrexate breakdown products are risk factors. The use of intrathecal Methotrexate is a reasonably safe and effective chemotherapeutic modality when proper administrative techniques are observed.
Methotrexate in dermatology
Dermatol Ther 2007 Jul-Aug;20(4):216-28.PMID:17970887DOI:10.1111/j.1529-8019.2007.00135.x.
Methotrexate is a folic acid analog pioneered for use in inflammatory diseases by dermatologists, and used successfully for over 40 years for a wide variety of cutaneous diseases. In addition to its antiproliferative properties, Methotrexate has other more recently recognized anti-inflammatory properties related to its effects on adenosine. Further research concerning its mechanism of action and genetic enzymatic variations suggest future possibilities for maximizing therapy and predicting adverse events. In this review the present authors will explore Methotrexate's pharmacokinetics, mode of administration, dosing guidelines, side effect profile, and medication interactions. In addition, the present authors hope to offer practical guidelines for dose initiation and adjustment, and to summarize new research on its mechanism of action and implications for future therapy.