Leflunomide (HWA486)

For research use only. Not for use in humans.

目录号:S1247 别名: RS-34821, SU101, Arava 中文名称:来氟米特

Leflunomide (HWA486) Chemical Structure

CAS No. 75706-12-6

Leflunomide (HWA486, RS-34821, SU101, Arava)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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1546.12 现货
RMB 1190.59 现货
RMB 3843.33 现货
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客户使用Selleck生产的Leflunomide (HWA486)发表文献9篇:

客户使用该产品的4个实验数据:

  • Peritoneal macrophages were pretreated for 1 h with the leflunomide (100 umol/L), followed by treatment with 10 ug/ml rTsP53 for 6 h. Western blot analysis of P-STAT6 and STAT6 expression was performed. Corresponding staining for b-actin was carried out to control for equal loading. *P < 0.05 versus control group, #P < 0.05 versus rTsP53 group.

    Cell Immunol 2014 288(1-2), 1-7. Leflunomide (HWA486) purchased from Selleck.

    Peritoneal macrophages were stained for FITC-MR. Flow cytometry analysis of MFI. The result for one representative of three independent experiments is shown.

    Cell Immunol 2014 288(1-2), 1-7. Leflunomide (HWA486) purchased from Selleck.

  • We found that the expression of Arg1, Ym1 and IL-10 on peritoneal macrophages incubated with leflunomide and rTsP53 were significantly down-regulated in comparison to treatment with rTsP53 alone.

    Cell Immunol 2014 288(1-2), 1-7. Leflunomide (HWA486) purchased from Selleck.

    H1299, H460, A549 cells were treated with leflunomide or teriflunomide at indicated concentrations for 24 h.

    Toxicol Lett, 2018, . Leflunomide (HWA486) purchased from Selleck.

产品安全说明书

Dehydrogenase抑制剂选择性比较

生物活性

产品描述 Leflunomide (HWA486, RS-34821, SU101, Arava)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。
靶点
Dihydroorotate dehydrogenase [1]
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
B-cells MlSySpVv[3Srb36gZZN{[Xl? M1X2WWlvKH[rdILvJIlvcGmkaYTpc44hd2ZiQXKg[o9zdWG2aX;uJIZzd21idILpcol1em:yaHXufYwudGmyb4DvcJl{[WOlaHHybYRmKCiWTmCtUHBUMSCELXPlcIx{NCCLQ{WwQVUvOc7:TR?= NEfWNJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUO4OFI1Oyd-MUGzPFQzPDN:L3G+
A673 M3fmeZFJXFNiYYPzZZk> NYm1NGdLeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= M1H4OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC NFnhcVZyUFSVIHHzd4F6 NXHh[G5CeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> MoLuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC NXTiOJFreUiWUzDhd5NigQ>? NIrnbIdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUy2QLV3DJINmdGy| NVrqO5B5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 29423085     


Leflunomide causes a dose-dependent decrease in cell viability in eight human melanoma cell lines. BRAFWT cell lines; M202 (blue), M285 (red), M375 (green) and M296 (purple). BRAFV600E mutant cell lines; A375 (orange), M229 (grey), SKmel28 (khaki) and SKmel5 (black). Cell viability was determined by using CellTiter-Glo reagent and all values are represented as a percentage (%) relative to the vehicle control. Data is presented as the mean ± SEM of three independent experiments each performed with cell culture triplicates. 

29423085
Western blot
DH0DH; 

PubMed: 23977077     


The DHODH protein expression levels were detected by western blotting in three neuroblastoma cell lines treated with either DMSO or 100 µM leflunomide for 72 hours. α-tubulin as the control.

ATF4 / CHOP ; 

PubMed: 29427785     


Glucose-grown and galactose-grown HepG2 cells were exposed to 50 to 300 μM of leflunomide for 6 h. Western blot showed that galactose-grown HepG2 cells exhibited more prominent increase in both ATF4 and CHOP protein levels. 

CDK2 / Cyclin A2 ; 

PubMed: 29348830     


Western blot assay was performed to assess the cell cycle-related protein levels in A375 and MV3 cells after treatment with leflunomide for 0, 24, 48, 72 and 96 hours. Tubulin was used as a loading control.

23977077 29427785 29348830
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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 54 mg/mL (199.84 mM)
Water Insoluble
Ethanol ''54 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 270.21
化学式

C12H9F3N2O2

CAS号 75706-12-6
储存条件 粉状
溶于溶剂
别名 RS-34821, SU101, Arava

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04212416 Recruiting Drug: Leflunomide 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 Recruiting Drug: Leflunomide COVID-19 University of Chicago May 5 2020 Phase 1
NCT03715699 Unknown status Drug: Prednisone|Drug: Prednisone and Leflunomide Autoimmune Disease Peking Union Medical College Hospital July 1 2018 Not Applicable
NCT03599986 Completed -- Active Rheumatoid Arthritis Eva Pharma|DataClin June 16 2017 --
NCT01500551 Recruiting Drug: Tofacitinib Juvenile Idiopathic Arthritis Pfizer March 18 2013 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID