Methotrexate (CL-14377)

製品コード:S1210 別名:NCI-C04671, Amethopterin, WR19039, abitrexate

For research use only.

Methotrexate (CL14377, MTX, NCI-C04671, Amethopterin, WR19039, abitrexate), analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.

Methotrexate (CL-14377)化学構造

CAS No. 59-05-2

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 24200
JPY 19100
JPY 50800

代表番号: 03-5615-9297|電子メール:[email protected]
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文献中Selleckの製品使用例(66)

製品安全説明書

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生物活性

製品説明 Methotrexate (CL14377, MTX, NCI-C04671, Amethopterin, WR19039, abitrexate), analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.
ターゲット
hDHFR [4]
(Activated peripheral T cells)
24 nM
体外試験

Methotrexate (0.1-10 mM) induces apoptosis of in vitro activated T cells from human peripheral blood. Methotrexate achieves clonal deletion of activated T cells in mixed lymphocyte reactions. Methotrexate can selectively delete activated peripheral blood T cells by a CD95-independent pathway. [1] Methotrexate is taken up by cells via the reduced folate carrier and then is converted within the cells to polyglutamates. Methotrexate leads to diminished production of leukotriene B4 by neutrophils stimulated ex vivo. Methotrexate polyglutamates inhibit the enzyme aminoimidazolecarboxamidoadenosineribonucleotide (AICAR) transformylase more potently than the other enzymes involved in purine biosynthesis. Methotrexate is also known to suppress TNF activity by suppressing TNF-induced nuclear factor-κB activation in vitro, in part related to a reduction in the degradation and inactivation of an inhibitor of this factor, IκBα, and probably related to the release of adenosine. Methotrexate suppresses the production of both TNF and IFN-γ by T-cell-receptor-primed T lymphocytes from both healthy human donors and RA patients. Methotrexate treatment is associated with a significant decrease of TNF-α-positive CD4+ T cells, while the number of T cells expressing the anti-inflammatory cytokine IL-10 increased. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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L1210 MlzESpVv[3Srb36gZZN{[Xl? Ml;RTY4hfmm2cn:gbY5pcWKrdHnvckBw\iCmaXj5[JJw\m:uYYTlJJJm\HWldHHz[UApTEiIUjmgbY4hVDF{MUCgZ4VtdHNuIFvpJF0hOC5yMECwNFQ5KM7:TT6= NInsU4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUCxNlI3Lz5zNUCxNlI3RC:jPh?=
L1210 NV3JdGhvTnWwY4Tpc44h[XO|YYm= NWS1cFNoUW6qaXLpeI9zgSCjY4Tpeol1gSCxZjDEbYh6\HKxZn;sZZRmKHKnZIXjeIF{\SCrbjDMNVIyOCClZXzsd{whU2liPTCwMlAxODByNEig{txONg>? NWTEPHRNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOEK3O|Q6Pyd-OEK3O|Q6PzxxYU6=
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CCRF-CEM MWrGeY5kfGmxbjDhd5NigQ>? MoDUTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JGRqcHmmcn;mc4xifGVicnXkeYN1[XOnIDjETGZTMSCrc3;sZZRm\CCocn;tJGNEWkZvQ1XNJIh2dWGwIHzleYtmdWmjIHPlcIx{KGmwIHX4dIVzcW2nboSgNUwhUUN3MDC9JFAvODByN{Kg{txONg>? NWXM[mRZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOEW2PFgzPyd-OEW2PFgzPzxxYU6=
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CCRF-CEM NF\kNXRHfW6ldHnvckBie3OjeR?= M2rWUGlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBFcWi7ZILv[o9t[XSnIILl[JVkfGG|ZTCoSGhHWiliaYPvcIF1\WRiZoLvcUBES1KILVPFUUBpfW2jbjDs[ZVs\W2rYTDj[YxteyCrbjDlfJBmemmvZX70JFEtKEmFNUCgQUAxNjByMUG4JO69VS5? NGjoNmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi96NU[4PFI4Lz56NU[4PFI4RC:jPh?=
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アッセイ
Methods Test Index PMID
Western blot ppJAK1 / ppJAK2 / JAK1 / JAK2 ; pSTAT1 / pSTAT3 / pSTAT5 / STAT1 / STAT3 / STAT5 ; AKT / p-AKT / mTOR / p-mTOR / Beclin 1 / HMGB1 26131691 26702616
体内試験 Methotrexate increases splenocyte AICAR content, raised adenosine concentrations in exudates from carrageenan-inflamed air pouches, and markedly inhibits leukocyte accumulation in inflamed air pouches in mice. Methotrexate-mediated reduction in leukocyte accumulation is partially reversed by injection of adenosine deaminase (ADA) into the air pouch, completely reverses by a specific adenosine A2 receptor antagonist, 3,7-dimethyl-1-propargylxanthine (DMPX), but not affected by an adenosine A1 receptor antagonist, 8-cyclopentyl-dipropylxanthine in mice. [3]

お薦めの試験操作(参考用のみ)

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。

5mg/mL

化学情報

分子量 454.44
化学式

C20H22N8O5

CAS No. 59-05-2
Storage 3年 -20°C
2年 -80°C in solvent
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

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04483466 Not yet recruiting Drug: Methotrexate|Drug: Placebo Investigate the Effect(s) of Methotrexate Treatment on Arthritis Disease Severity George Washington University July 1 2022 Phase 3
NCT03642795 Recruiting Other: Questionnaire Rheumatoid Polyarthritis Centre Hospitalier Universitaire de Nīmes June 23 2022 --
NCT05370690 Not yet recruiting -- Uveitis University Hospital Brest May 1 2022 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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Tags: Methotrexate (CL-14377)を買う | Methotrexate (CL-14377) ic50 | Methotrexate (CL-14377)供給者 | Methotrexate (CL-14377)を購入する | Methotrexate (CL-14377)費用 | Methotrexate (CL-14377)生産者 | オーダーMethotrexate (CL-14377) | Methotrexate (CL-14377)化学構造 | Methotrexate (CL-14377)分子量 | Methotrexate (CL-14377)代理店