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Leflunomide

来氟米特
Catalog No.
A2852
AHR激动剂,免疫抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 727.00
现货
100mg
¥ 909.00
现货

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A

背景

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.

文献引用

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt270.21
Cas No.75706-12-6
FormulaC12H9F3N2O2
Solubility≥83.33 mg/mL in DMSO; insoluble in H2O; ≥18.57 mg/mL in EtOH
Chemical Name5-methyl-N-[4-(trifluoromethyl)phenyl]-1,2-oxazole-4-carboxamide
SDFDownload SDF
Canonical SMILESCC1=C(C=NO1)C(=O)NC2=CC=C(C=C2)C(F)(F)F
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试验操作

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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