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Leflunomide
別名：HWA486, RS-34821, SU101
Leflunomide is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR.
CAS No. 75706-12-6
文献中Selleckの製品使用例（17）
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製品安全説明書
現在のバッチを見る：
純度：
99.93%
99.93
Leflunomide関連製品
シグナル伝達経路
Dehydrogenase阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| B-cells | Function assay | In vitro inhibition of Ab formation from trinitrophenyl-lipopolysaccharide (TNP-LPS) B-cells, IC50=5.1μM | 11384243 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | Leflunomide is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR. | |
|---|---|---|
| Targets |
|
| In Vitro | ||||
| In vitro | Leflunomide is actually a prodrug that is processed in vivo to the active metabolite A771726，which has been shown to inhibit proliferation of mononuclear and T-cells. Leflunomide is an inhibitor of several protein tyrosine kinases, with IC50 values between 30 mM and 100 mM in vitro cellular and enzymatic assays. [1] Leflunomide is capable of inhibiting anti-CD3- and interleukin-2 (IL-2)-stimulated T cell proliferation. Leflunomide is able to inhibit p59fyn and p56lck activity in in vitro tyrosine kinase assays. Leflunomide also inhibits Ca2+ mobilization in Jurkat cells stimulated by anti-CD3 antibody but not in those stimulated by ionomycin. Leflunomide also inhibits distal events of anti-CD3 monoclonal antibody stimulation, namely, IL-2 production and IL-2 receptor expression on human T lymphocytes. Leflunomide also inhibits tyrosine phosphorylation in CTLL-4 cells stimulated by IL-2. [2] Leflunomide is an immunomodulatory drug that may exert its effects by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH), which plays a key role in the de novo synthesis of the pyrimidine ribonucleotide uridine monophosphate (rUMP). Leflunomide prevents the expansion of activated and autoimmune lymphocytes by interfering with the cell cycle progression due to inadequate production of rUMP and utilizing mechanisms involving p53. [3] | |||
|---|---|---|---|---|
| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Growth inhibition assay | Cell viability |
|
29423085 | |
| Western blot | DH0DH ATF4 / CHOP CDK2 / Cyclin A2 |
|
23977077 | |
| In Vivo | ||
| In Vivo | Leflunomide is able to prevent and reverse allograft and xenograft rejection in rodents, dogs, and monkeys. [2] | |
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05605587 | Recruiting | MEN1 Gene Mutation |
University Hospital Basel Switzerland |
May 2 2023 | Not Applicable |
| NCT04212416 | Active not recruiting | Chronic Graft Versus Host Disease|Steroid Refractory Graft Versus Host Disease |
City of Hope Medical Center|National Cancer Institute (NCI) |
May 12 2020 | Phase 1 |
| NCT04361214 | Terminated | COVID-19 |
University of Chicago |
May 5 2020 | Phase 1 |
| NCT03715699 | Unknown status | Autoimmune Disease |
Peking Union Medical College Hospital |
July 1 2018 | Not Applicable |
| NCT03599986 | Completed | Active Rheumatoid Arthritis |
Eva Pharma|DataClin |
June 16 2017 | -- |
化学情報
| 分子量 | 270.21 | 化学式 | C12H9F3N2O2 |
| CAS No. | 75706-12-6 | SDF | Download Leflunomide SDFをダウンロードする |
| Smiles | CC1=C(C=NO1)C(=O)NC2=CC=C(C=C2)C(F)(F)F | ||
| 保管 | |||
|
In vitro |
DMSO : 54 mg/mL ( (199.84 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Ethanol : 54 mg/mL Water : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
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
匹
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。
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