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

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

目錄號: HY-B0083 純度: 99.82%
COA 產(chǎn)品使用指南 技術(shù)支持

Leflunomide 是一種嘧啶合成抑制劑，通過抑制二氫乳清酸脫氫酶 (DHODH) 起作用，具有抗風(fēng)濕的作用。

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Leflunomide Chemical Structure

Leflunomide Chemical Structure

CAS No. : 75706-12-6

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規(guī)格 價(jià)格 是否有貨 數(shù)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   詢價(jià)  
5 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Leflunomide:

    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

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

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

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HepG2 IC50
    109.5 μM
    Compound: Leflunomide
    Cytotoxicity against human HepG2 cells assessed as reduction in glucose induced mitochondrial toxicity by measuring ATP depletion incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    Cytotoxicity against human HepG2 cells assessed as reduction in glucose induced mitochondrial toxicity by measuring ATP depletion incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    		[PMID: 32942072]
    HT-1080 IC50
    30 μM
    Compound: Leflunomide
    Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay
    Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay
    		[PMID: 33007554]
    HT-1080 IC50
    38 μM
    Compound: Leflunomide
    Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay
    Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay
    		[PMID: 33007554]
    HT-29 IC50
    75 μM
    Compound: Leflunomide
    Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay
    Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay
    		[PMID: 33007554]
    HT-29 IC50
    75 μM
    Compound: Leflunomide
    Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay
    Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay
    		[PMID: 33007554]
    M21 IC50
    83 μM
    Compound: Leflunomide
    Antiproliferative activity against human M21 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay
    Antiproliferative activity against human M21 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay
    		[PMID: 33007554]
    M21 IC50
    83 μM
    Compound: Leflunomide
    Antiproliferative activity against human M21 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay
    Antiproliferative activity against human M21 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay
    		[PMID: 33007554]
    MCF7 IC50
    55 μM
    Compound: Leflunomide
    Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay
    Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay
    		[PMID: 33007554]
    MCF7 IC50
    57 μM
    Compound: Leflunomide
    Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay
    Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay
    		[PMID: 33007554]
    體外研究
    (In Vitro)

    Leflunomide 實(shí)際上是一種前體藥物，已被證明可以抑制單核細(xì)胞和 T 細(xì)胞的增殖。Leflunomide 是幾種蛋白酪氨酸激酶的抑制劑，體外細(xì)胞和酶促測定的 IC50 值介于 30 mM 和 100 mM 之間[1]。
    Leflunomide 能夠抑制抗 CD3 和白細(xì)胞介素 2 (IL-2) 刺激的 T 細(xì)胞增殖。Leflunomide 能夠在體外酪氨酸激酶測定中抑制 p59fyn 和 p56lck 活性。Leflunomide 還抑制抗 CD3 抗體刺激的 Jurkat 細(xì)胞中的 Ca2+ 動員，但不會抑制離子霉素刺激的 Jurkat 細(xì)胞中的 Ca2+ 動員。Leflunomide 還抑制抗 CD3 單克隆抗體刺激的遠(yuǎn)端事件，即 IL-2 的產(chǎn)生和人類 T 淋巴細(xì)胞上的 IL-2 受體表達(dá)。Leflunomide 還抑制 IL-2 刺激的 CTLL-4 細(xì)胞中的酪氨酸磷酸化[2]。
    Leflunomide 是一種免疫調(diào)節(jié)藥物，可能通過抑制線粒體酶二氫乳清酸脫氫酶 (DHODH) 發(fā)揮作用，而該酶在嘧啶核苷酸尿苷單磷酸 (rUMP) 的從頭合成中起著關(guān)鍵作用。Leflunomide 通過干擾因 rUMP 生成不足而導(dǎo)致的細(xì)胞周期進(jìn)程并利用涉及 p53 的機(jī)制來阻止活化和自身免疫淋巴細(xì)胞的擴(kuò)增[3]。

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

    270.21

    Formula

    C12H9F3N2O2
    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    來氟米特；來氟洛米
    結(jié)構(gòu)分類
    初始來源
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : ≥ 50 mg/mL (185.04 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實(shí)驗(yàn)：

    請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (9.25 mM); 懸濁液; 超聲加熱助溶

      此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

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

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    動物溶解方案計(jì)算器
    請輸入動物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.82%

    參考文獻(xiàn)
    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.
    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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
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    產(chǎn)品名稱：
    Leflunomide
    目錄號：
    HY-B0083
    需求量：