Leflunomide

製品コードS1247 バッチS124703

印刷

化学情報

Chemical Structure Synonyms HWA486, RS-34821, SU101 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C12H9F3N2O2
分子量 270.21 CAS No. 75706-12-6
Solubility (25°C)* 体外 DMSO 54 mg/mL (199.84 mM)
Ethanol 54 mg/mL (199.84 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 5.000mg/ml (18.50mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 5.000mg/ml (18.50mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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.
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. This compound is an inhibitor of several protein tyrosine kinases, with IC50 values between 30 mM and 100 mM in vitro cellular and enzymatic assays. [1] It is capable of inhibiting anti-CD3- and interleukin-2 (IL-2)-stimulated T cell proliferation. This drug is able to inhibit p59fyn and p56lck activity in in vitro tyrosine kinase assays. It also inhibits Ca2+ mobilization in Jurkat cells stimulated by anti-CD3 antibody but not in those stimulated by ionomycin. This compound also inhibits distal events of anti-CD3 monoclonal antibody stimulation, namely, IL-2 production and IL-2 receptor expression on human T lymphocytes. It also inhibits tyrosine phosphorylation in CTLL-4 cells stimulated by IL-2. [2] This immunomodulatory drug 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). It 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]
in vivo Leflunomide is able to prevent and reverse allograft and xenograft rejection in rodents, dogs, and monkeys. [2]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/8573583/
  • https://pubmed.ncbi.nlm.nih.gov/7759480/
  • https://pubmed.ncbi.nlm.nih.gov/10600330/
  • https://pubmed.ncbi.nlm.nih.gov/16904479/

カスタマーフィードバック

Data from [Cell Immunol, 2014, 288(1-2), 1-7]

Data from [Cell Immunol, 2014, 288(1-2), 1-7]

Data from [Cell Immunol, 2014, 288(1-2), 1-7]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Proteogenomic characterization of non-functional pancreatic neuroendocrine tumors unravels clinically relevant subgroups [ Cancer Cell, 2025, 43(4):776-796.e14] PubMed: 40185092
Targeting the MARCH5-MFN2 axis to enhance mitochondrial fusion and sensitize multiple myeloma cells to venetoclax [ J Transl Med, 2025, 23(1):917] PubMed: 40814067
Vaccinia growth factor-dependent modulation of the mTORC1-CAD axis upon nutrient restriction [ J Virol, 2025, 99(2):e0211024] PubMed: 39817770
Coronavirus envelope protein activates TMED10-mediated unconventional secretion of inflammatory factors [ Nat Commun, 2024, 15(1):8708] PubMed: 39379362
Role of vaccinia virus growth factor in stimulating the mTORC1-CAD axis of the de novo pyrimidine pathway under different nutritional cues [ bioRxiv, 2024, 2024.07.02.601567] PubMed: 39005450
IDH2 stabilizes HIF-1α-induced metabolic reprogramming and promotes chemoresistance in urothelial cancer [ EMBO J, 2023, e110620.] PubMed: 36637036
Role of mitochondrial fusion proteins MFN2 and OPA1 on lung cellular senescence in chronic obstructive pulmonary disease [ Respir Res, 2023, 24(1):319] PubMed: 38110986
Dihydroorotate dehydrogenase promotes cell proliferation and suppresses cell death in esophageal squamous cell carcinoma and colorectal carcinoma [ Transl Cancer Res, 2023, 12(9):2294-2307] PubMed: 37859742
Dihydroorotate dehydrogenase promotes cell proliferation and suppresses cell death in esophageal squamous cell carcinoma and colorectal carcinoma [ Transl Cancer Res, 2023, 12(9):2294-2307] PubMed: 37859742
De novo pyrimidine synthesis fuels glycolysis and confers chemoresistance in gastric cancer [ Cancer Lett, 2022, S0304-3835(22)00321-4] PubMed: 35921972

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。