2. Metabolic Enzyme/Protease Anti-infection
  3. Dihydroorotate Dehydrogenase Endogenous Metabolite Bacterial
  4. Leflunomide

Leflunomide  (Synonyms: 来氟米特; HWA486; RS-34821; SU101)

目录号: HY-B0083 纯度: 99.82%
COA 产品使用指南

摩尔计算器

Leflunomide 是一种嘧啶合成抑制剂，通过抑制二氢乳清酸脱氢酶 (DHODH) 起作用，具有抗风湿的作用。

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Leflunomide Chemical Structure

Leflunomide Chemical Structure

CAS No. : 75706-12-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥693
In-stock
50 mg ￥630
In-stock
100 mg ￥950
In-stock
500 mg ￥2600
In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Leflunomide:

Leflunomide 相关抗体

Top Publications Citing Use of Products

    Leflunomide purchased from MCE. Usage Cited in: Haematologica. 2018 Sep;103(9):1472-1483.  [Abstract]

    Western blot analysis the changes of apoptosis-associated protein at day 18 of HL60 xenograft tumors treated with vehicle, Isobavachalcone (IBC) or Leflunomide (LEF). Expression levels of MYC and p21 in vehicle, IBC, or LEF treated tumors are estimated by western blot.

    Leflunomide purchased from MCE. Usage Cited in: Cancer Lett. 2018 Mar 28;417:21-34.  [Abstract]

    Western blot indicates that the expression of pSTAT6 and CCL26 in HCC cells induced by ectopic NDRG1 expression is obviously attenuated by LEF treatment.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase (DHODH), and acts as a disease-modifying antirheumatic agent.

    体外研究
    (In Vitro)

    Leflunomide is actually a prodrug that has been shown to inhibit proliferation of mononuclear and T-cells. Leflunomide is an inhibitor of several protein tyrosine kinases, with IC50 values between 30 mM and 100 mM in vitro cellular and enzymatic assays[1].
    Leflunomide is capable of inhibiting anti-CD3- and interleukin-2 (IL-2)-stimulated T cell proliferation. Leflunomide is able to inhibit p59fyn and p56lck activity in in vitro tyrosine kinase assays. Leflunomide also inhibits Ca2+ mobilization in Jurkat cells stimulated by anti-CD3 antibody but not in those stimulated by ionomycin. Leflunomide also inhibits distal events of anti-CD3 monoclonal antibody stimulation, namely, IL-2 production and IL-2 receptor expression on human T lymphocytes. Leflunomide also inhibits tyrosine phosphorylation in CTLL-4 cells stimulated by IL-2[2].
    Leflunomide is an immunomodulatory drug that 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). Leflunomide 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Leflunomide 相关抗体:
    Clinical Trial
    分子量

    270.21

    Formula

    C12H9F3N2O2
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    来氟米特；来氟洛米
    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 50 mg/mL (185.04 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.7008 mL 18.5041 mL 37.0083 mL
    5 mM 0.7402 mL 3.7008 mL 7.4017 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (9.25 mM); 悬浊液; 超声加热助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (9.25 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.82%

    COA (288 KB) LCMS (93 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    DHODase activity is measured by the DCIP colorimetric assay. This is a coupled assay in which oxidation of DHO and subsequent reduction of ubiquinone are stoichiometrically equivalent to the reduction of DCIP. Reduction of DCIP is accompanied by a loss of absorbance at 610 nm (ε=21500 M/cm). The assay is performed in a 96-well microtiter plate at ambient temperature (ca. 25°C). Stock solutions of 10 mM leflunomide and A771726 are prepared in dimethyl sulfoxide (DMSO) and these are diluted with reaction buffer (100 mM Tris and 0.1 % Triton X-100, pH 8.0) to prepare working stocks of the inhibitors at varying concentrations. For each reaction, the well contained 10 nM DHODase, 68 μM DCIP, 0.16 mg/mL gelatin, the stated concentration of ubiquinone, 10 μL of an inhibitor working stock to give the stated final concentration, and reaction buffer. After a 5-min equilibration period, the reaction is initiated by addition of DHO to the stated final concentrations. The total volume of reaction mixture for each assay is 150 μL, and the final DMSO concentration is ≤ 0.01% (v/v). The reaction progress is followed by recording the loss of absorbance at 610 nm over a 10-min period (during which the velocity remained linear). Velocities are reported as the change in absorbance at 610 nm per minute, and each reported value is the average of three replicates. In experiments where the DHO or ubiquinone concentration is varied, the other substrate is held constant at 200 μM. To determine the inhibitor potency of leflunomide and A771726, the effects of varying concentrations of the two compounds on the initial velocity of the DHODase reaction is measured over a concentration range of 0.01−1.0 μM. In these experiments the DHO and ubiquinone concentrations are held constant at 200 and 100 μM, respectively.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Leflunomide 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.7008 mL 18.5041 mL 37.0083 mL 92.5206 mL
    5 mM 0.7402 mL 3.7008 mL 7.4017 mL 18.5041 mL
    10 mM 0.3701 mL 1.8504 mL 3.7008 mL 9.2521 mL
    15 mM 0.2467 mL 1.2336 mL 2.4672 mL 6.1680 mL
    20 mM 0.1850 mL 0.9252 mL 1.8504 mL 4.6260 mL
    25 mM 0.1480 mL 0.7402 mL 1.4803 mL 3.7008 mL
    30 mM 0.1234 mL 0.6168 mL 1.2336 mL 3.0840 mL
    40 mM 0.0925 mL 0.4626 mL 0.9252 mL 2.3130 mL
    50 mM 0.0740 mL 0.3701 mL 0.7402 mL 1.8504 mL
    60 mM 0.0617 mL 0.3084 mL 0.6168 mL 1.5420 mL
    80 mM 0.0463 mL 0.2313 mL 0.4626 mL 1.1565 mL
    100 mM 0.0370 mL 0.1850 mL 0.3701 mL 0.9252 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Leflunomide75706-12-6HWA486 RS-34821 SU101来氟米特来氟洛米HWA 486HWA-486RS34821RS 34821RS-34821SU101SU 101SU-101Dihydroorotate DehydrogenaseEndogenous MetaboliteBacterialDHODHInhibitorinhibitorinhibit

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