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别名 | HWA486, RS-34821, SU101 | 储存条件 (自收到货起) |
3年 / -20°C / 粉状 1年 / -80°C / 溶于溶剂 |
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化学式 | C12H9F3N2O2 |
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分子量 | 270.21 | CAS号 | 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(现配现用) |
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* <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. |
产品描述 | Leflunomide是一种属于DMARD的免疫抑制剂,可抑制嘧啶的合成和 protein tyrosine kinase 的活性。Leflunomide 的活性代谢产物为A77 1726(RS-61980),可抑制 dihydroorotate dehydrogenase (DHODH)。Leflunomide 还是 AhR 的激动剂。 | |
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靶点 |
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体外研究 | Leflunomide实际上是药物前体,在体内加工成活性代谢物A771726,这已被证明能抑制单核细胞和T细胞的增殖。Leflunomide是几种蛋白酪氨酸激酶的抑制剂,在体外的细胞和酶测定中IC50值在30 mM和100 mM之间。[1] Leflunomide能够抑制抗CD3-和白细胞介素-2(IL-2)刺激的T细胞增殖。在体外酪氨酸激酶测定中,Leflunomide能够抑制p59fyn和p56lck活性。Eflunomide也抑制Jurkat细胞中抗CD3抗体刺激的钙动员,而不影响ionomycin刺激的钙动员。Leflunomide也抑制抗CD3单克隆抗体刺激的反应,如人T淋巴细胞中IL-2产生和IL-2受体表达。Leflunomide也抑制CTLL-4细胞中IL-2刺激的酪氨酸磷酸化. [2] Leflunomide是一种免疫调节药物可通过抑制线粒体酶二氢乳清脱氢酶(DHODH)发挥作用,它在从头合成的嘧啶核糖核苷酸尿苷一磷酸的过程中发挥关键作用。由于生产rUMP的不足和涉及p53的机制,Leflunomide通过细胞周期进程的干扰防止激活与自身免疫性淋巴细胞的扩大。[3] | |
体内研究 | 在啮齿动物,狗,猴等中,Leflunomide能够防止和逆转同种异体移植物和异种移植物排斥。[2] |
数据来源于[, 288(1-2), 1-7]
数据来源于[, 288(1-2), 1-7]
数据来源于[, 288(1-2), 1-7]
数据来源于[Data independently produced by , , Toxicol Lett, 2018, ]
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 |
UBE2T-mediated Akt ubiquitination and Akt/β-catenin activation promotes hepatocellular carcinoma development by increasing pyrimidine metabolism [ Cell Death Dis, 2022, 13(2):154] | PubMed: 35169125 |
Therapeutic targeting of both dihydroorotate dehydrogenase and nucleoside transport in MYCN-amplified neuroblastoma [ Cell Death Dis, 2021, 12(9):821] | PubMed: 34462431 |
Exosome-Depleted Excretory-Secretory Products of the Fourth-Stage Larval Angiostrongylus cantonensis Promotes Alternative Activation of Macrophages Through Metabolic Reprogramming by the PI3K-Akt Pathway [ Front Immunol, 2021, 12:685984] | PubMed: 34367145 |
In vitro evaluation of disease-modifying antirheumatic drugs against rheumatoid arthritis associated pathogens of the oral microflora [ RMD Open, 2021, 7(3)e001737] | PubMed: 34588273 |
Leflunomide Inhibits rat-to-Mouse Cardiac Xenograft Rejection by Suppressing Adaptive Immune Cell Response and NF-κB Signaling Activation [ Cell Transplant, 2021, 30:9636897211054503] | PubMed: 34814739 |
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