规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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10mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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5g |
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10g |
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Other Sizes |
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体外研究 (In Vitro) |
体外活性:甲氨蝶呤 (0.1-10 mM) 诱导人外周血体外活化 T 细胞凋亡。甲氨蝶呤在混合淋巴细胞反应中实现活化 T 细胞的克隆删除。甲氨蝶呤可以通过 CD95 独立途径选择性地删除活化的外周血 T 细胞。甲氨蝶呤通过还原叶酸载体被细胞吸收,然后在细胞内转化为聚谷氨酸盐。甲氨蝶呤会导致离体刺激的中性粒细胞产生的白三烯 B4 减少。甲氨蝶呤聚谷氨酸盐比其他参与嘌呤生物合成的酶更有效地抑制氨基咪唑羧酰胺腺苷核糖核苷酸 (AICAR) 转化酶。甲氨蝶呤还已知通过在体外抑制 TNF 诱导的核因子 -κB 激活来抑制 TNF 活性,部分与减少该因子抑制剂 IκBα 的降解和失活有关,并且可能与腺苷的释放有关。甲氨蝶呤抑制来自健康人类供体和 RA 患者的 T 细胞受体引发的 T 淋巴细胞产生 TNF 和 IFN-γ。甲氨蝶呤治疗与 TNF-α 阳性 CD4+ T 细胞显着减少有关,而表达抗炎细胞因子 IL-10 的 T 细胞数量增加。细胞测定:使用 96 孔微量滴定板在生长抑制实验中研究每种细胞系。由于 antifols 具有时间表依赖性,初步实验旨在确定最长的暴露持续时间,从而允许细胞连续对数期生长而不改变培养基,同时保持 SRB 光密度和细胞数量之间的线性关系。细胞铺板后 24 小时,将细胞系暴露于 antifol 中 120 小时(每个实验重复 3 次)。为了确保可以观察到完整的 S 形生存浓度曲线,研究了以下药物浓度:甲氨蝶呤 (0.002-5 μM)、AMT (0.0001-1 μM)、PXD (0.0003-10 μM)、TLX (0.0002-0.5)微米)。实验至少重复两次。
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体内研究 (In Vivo) |
氨甲喋呤或甲氨蝶呤可降低小鼠的胸腺和脾脏指数。剂量≥5 mg/kg时,甲氨蝶呤显着减少脾脏、胸腺和白细胞。然而,模型组和治疗加对照组差异显着(p <0.01)。很明显,葡萄籽原花青素与西伯利亚人参刺五加苷一起给药可减少甲氨蝶呤对小鼠胸腺和脾脏指数的负面影响[2]。甲氨蝶呤 (MTX)(2 毫克/公斤;腹膜内注射;每周一次)持续五周,可有效治疗弗氏完全佐剂诱发的关节炎。姜黄素(30 mg/kg 和 100 mg/kg,每周 3 次,持续五周;腹腔注射)和甲氨蝶呤(1 mg/kg;腹腔注射;每周一次,持续五周)一起具有很强的抗关节炎作用和保护作用。抗血液毒性[4]。
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动物实验 |
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参考文献 |
[1]. Tian H, et al. Understanding the mechanisms of action of methotrexate: implications for the treatment of rheumatoid arthritis. Bull NYU Hosp Jt Dis. 2007;65(3):168-73.
[2]. Swierkot J, et al. Methotrexate in rheumatoid arthritis. Pharmacol Rep. 2006 Jul-Aug;58(4):473-92. [3]. Ehab Tousson, et al. The Effect of L-carnitine on Amethopterin-induced Toxicity in Rat Large Intestine. [4]. Banji D, et al. Evaluation of the concomitant use of methotrexate and curcumin on Freund's complete adjuvant-induced arthritis and hematological indices in rats. Indian J Pharmacol. 2011;43(5):546-550 |
分子式 |
C20H22N8O5
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分子量 |
454.44
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CAS号 |
59-05-2
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相关CAS号 |
Methotrexate disodium;7413-34-5;Methotrexate hydrate;133073-73-1;Methotrexate monohydrate;6745-93-3;Methotrexate-d3;432545-63-6
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SMILES |
O=C(O)[C@@H](NC(C1=CC=C(N(CC2=NC3=C(N)N=C(N)N=C3N=C2)C)C=C1)=O)CCC(O)=O
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InChi Key |
FBOZXECLQNJBKD-ZDUSSCGKSA-N
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InChi Code |
InChI=1S/C20H22N8O5/c1-28(9-11-8-23-17-15(24-11)16(21)26-20(22)27-17)12-4-2-10(3-5-12)18(31)25-13(19(32)33)6-7-14(29)30/h2-5,8,13H,6-7,9H2,1H3,(H,25,31)(H,29,30)(H,32,33)(H4,21,22,23,26,27)/t13-/m0/s1
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化学名 |
(S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioic acid.
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别名 |
alphamethopterin; amethopterin; methylaminopterin; CL 14377; NCIC04671; WR19039; WR-19039; WR 19039; MTX; NCI-C04671; NCI C04671; CL14377; CL-14377; Methotrexate.
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.50 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (5.50 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: 2% DMSO+30% PEG 300+5% Tween 80+ddH2O:5 mg/mL 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 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 | 4.4010 mL | |
10 mM | 0.2201 mL | 1.1003 mL | 2.2005 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT06123403 | Not yet recruiting | Diagnostic Test: blood methotrexate level and Cystatin C level |
Methotrexate Toxicity | Sohag University | January 2024 | |
NCT06108453 | Enrolling by invitation | Drug: Methotrexate Sodium Drug: Rifampicin |
Drug Interactions | Seoul National University Bundang Hospital |
August 21, 2023 | Phase 1 |
NCT03757364 | Completed | Drug: Methotrexate | Nail Psoriasis | Ryszard Górecki | January 7, 2018 | Ryszard Górecki |
NCT04483466 | Enrolling by invitation | Drug: Methotrexate Drug: Placebo |
Investigate the Effect(s) of Methotrexate Treatment on Arthritis Disease Severity |
George Washington University | July 18, 2023 | Phase 3 |
Effect of the combination of methotrexate and curcumin on mean body weight in arthritic rats. Values are mean ± SEM, n = 6, FCA-Freund's complete adjuvant, *P < 0.05 as compared with positive control td> |
Effect of methotrexate and curcumin treatment on blood indices in arthritic rats (n = 6). Values are mean ± SEM, FCA-Freund's complete adjuvant, *P < 0.05 compared with positive control td> |
Changes in MDA, GSH, total protein and catalase levels in large intestine in different groups under study. Data are expressed as mean ± S.E.M of 10 observations. Significant difference from the control group (G1) at *p<0.05. Significant difference from Amethopterin group (G3) at #p<0.05. Where G1, Control group; G2, L-carnitine group; G3, Amethopterin group; G4, Co-treated Amethopterin group with L-carnitine; G5, Post-treated Amethopterin group with L-carnitine; G6, Self-treated Amethopterin group td> |