| CAS NO: | 75706-12-6 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 100mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 270.21 |
| Cas No. | 75706-12-6 |
| Formula | C12H9F3N2O2 |
| Solubility | ≥83.33 mg/mL in DMSO; insoluble in H2O; ≥18.57 mg/mL in EtOH |
| Chemical Name | 5-methyl-N-[4-(trifluoromethyl)phenyl]-1,2-oxazole-4-carboxamide |
| Canonical SMILES | CC1=C(C=NO1)C(=O)NC2=CC=C(C=C2)C(F)(F)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Leflunomide（来氟米特）是芳香烃受体（AHR）的激动剂[1]。Leflunomide是可以口服的免疫调节剂。A771726（teriflunomide）是由leflunomide形成的非酶促活性药[2]。
研究表明，Leflunomide可以增加外周血和干细胞亚群的Tregs水平，增加这些细胞向受损的肾的迁移。在缺血再灌注肾中，Leflunomide可以增加细胞IL-10的表达，减少IL-17和IL-23的表达[1]。
在雄性脓毒症Wistar大白鼠中，Leflunomide显著降低脂质过氧化。同时，leflunomide成功地抑制肠中蛋白质羰基和NO的增加[2]。在人MTC-TT细胞中，Leflunomide以剂量和时间依赖的方式减少细胞增殖，抑制肿瘤标志物表达以及下调神经内分泌标记物ASCL1的蛋白表达[3]。
参考文献：
[1] Baban B1,Liu JY,Mozaffari MS. Aryl hydrocarbon receptor agonist, leflunomide, protects the ischemic-reperfused kidney: role of Tregs and stem cells. Am J Physiol Regul Integr Comp Physiol.2012 Dec;303(11):R1136-46.
[2] Ozturk E1,Surucu M2,Karaman A3,SamdancE4,Fadillioglu E5. Protective effect of leflunomideagainstoxidative intestinal injury in a rodent model of sepsis. J Surg Res.2014 Apr;187(2):610-5.
[3] Alhefdhi A1,Burke JF,Redlich A,Kunnimalaiyaan M,Chen H. Leflunomidesuppresses growth in human medullary thyroid cancer cells. J Surg Res.2013 Nov;185(1):212-6.
| Cell experiment:[1] | |
Cell lines | Human medullary thyroid cancer cell line TT (MTC-TT cells) |
Reaction Conditions | 75 ~ 150 μmol/L leflunomide for 2, 4, or 6 d incubation |
Applications | Leflunomide treatment down-regulated neuroendocrine markers achaete-scute complex-like 1 (ASCL1) and chromogranin A. Moreover, leflunomide significantly inhibited the growth of MTC-TT cells in a dose- and time- dependent manner. |
| Animal experiment:[2] | |
Animal models | Male C57BL/6 mice (10 ~ 12 wk of age) |
Dosage form | 40 mg/kg Injected intraperitoneally16 h prior to the induction of renal ischemic reperfusion insult |
Applications | Leflunomide treatment increased regulatory T cells and IL-10-positive cells but reduced IL-17- and IL-23-expressing cells in both the peripheral blood and kidney cells, indicative of down-regulation of inflammatory responses. Leflunomide treatment also increased mobilization of stems cells subsets in the peripheral blood and promoted their recruitment into the ischemic-reperfused kidney. Eventually, leflunomide treatment was able to preserve mitochondrial membrane potential as well as decrease apoptosis and necrosis of renal cells. |
Note | The technical data provided above is for reference only. |
References: 1. Alhefdhi A, Burke JF, Redlich A, et al. Leflunomide suppresses growth in human medullary thyroid cancer cells. Journal of Surgical Research, 2013, 185(1): 212-216. 2. Baban B, Liu JY, Mozaffari MS. Aryl hydrocarbon receptor agonist, leflunomide, protects the ischemic-reperfused kidney: role of Tregs and stem cells. American Journal of Physiology - Regulatory, Integrative and Comparative Physiology, 2012, 303(11): R1136-1146. | |
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