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  2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. GW0742

GW0742 是一種有效的 PPARβ 和 PPARδ 激動劑，在蛋白質(zhì)結(jié)合實(shí)驗(yàn)中，對人 PPARδ 的 IC50 值為 1 nM；同時對人 PPARδ，PPARα 和 PPARγ 的 EC50 值分別為 1 nM，1.1 μM 和 2 μM。

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GW0742 Chemical Structure

GW0742 Chemical Structure

CAS No. : 317318-84-6

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥660
In-stock
5 mg ￥598
In-stock
10 mg ￥950
In-stock
50 mg ￥2950
In-stock
100 mg ￥4538
In-stock
200 mg   詢價  
500 mg   詢價  

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Customer Review

    GW0742 purchased from MCE. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Oct;1864(10):3322-3338.  [Abstract]

    LAZ3 knock-down decreases NRF2 expression and nuclear translocation, while only the PPARa agonist (GW7647) can prevent this inhibition. Both PPARγ agonist (GW1929) and PPARδ agonist (GW0742) can not reverse these inhibitions.

    查看 PPAR 亞型特異性產(chǎn)品:

    • 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

    GW0742 is a potent PPARβ and PPARδ agonist, with an IC50 of 1 nM for human PPARδ in binding assay, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.

    IC50 & Target[1]

    PPARδ

    1 nM (EC50)

    PPARα

    1.1 μM (EC50)

    PPARγ

    2 μM (EC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CV-1 EC50
    ≤ 5.8 nM
    Compound: GW-0742
    Agonist activity at mouse PPAR-delta expressed in african green monkey CV-1 cells after 24 hrs by luciferase reporter gene assay
    Agonist activity at mouse PPAR-delta expressed in african green monkey CV-1 cells after 24 hrs by luciferase reporter gene assay
    		[PMID: 21074432]
    HEK293 EC50
    13 nM
    Compound: GW0742
    Transactivation of GAL4-fused human PPARdelta LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay
    Transactivation of GAL4-fused human PPARdelta LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay
    		[PMID: 30605833]
    體外研究
    (In Vitro)

    GW0742 is a potent PPARβ and PPARδ agonist, with an IC50 of 1 nM for human PPARδ, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ respectively[1]. GW0742 (100 μM) activates human PPARα and mouse PPARβ in MCF-7 cells. GW0742 (100 μM) significantly reduces low-KCl-induced apoptosis of cerebellar granule neurons. GW0742 shows no obvious inherent toxicity on cerebellar granule neuronal cells after treatment of 3-100 μM for 24 h, but induces increased cell death at 100 μM after 48 hr of treatment. Moreover, GW0742 (100 μM) increases c-Jun expression in cerebellar granule neuron cultures observed at 6 hr[2]. GW0742 (1 μM) induces PPARδ protein in neonatal rat cardiomyocytes. GW0742 also raises mRNA levels of long-chain acyl-CoA dehydrogenase (LCAD), very long-chain acyl-CoA dehydrogenase (VLCAD), acyl-CoA oxidase 1 (ACOX1), uncoupling protein 3 (UCP3), malonyl-CoA decarboxylase (MCD), and pyruvate dehydrogenase kinase 4 (PDK4) in neonatal rat cardiomyocytes[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    GW0742 (0.3 mg/kg, i.p.) reduces intensity masson-trichrome staining, and attenuates the histological signs in bleomycin instillatio (BLEO)-induced lung injury of mice. GW0742 (0.3 mg/kg, i.p.) also causes a reduction of the BLEO-induced loss body weight, and a decrease of myeloperoxidase (MPO) activity. GW0742 shows significant inhibition of TNF-a and IL-1β in instilled-mice. GW0742 prevents bleomycin-induced IkB-a degradation, reduces the levels of NF-kB p65 in the lung, and decreases iNOS and p-ERK expression in BLEO-induced mice[3]. GW0742 (5 mg/kg/day, i.v.) increases PPARδ protein level in the heart of rats. GW0742 also induces the increase in LCAD, VLCAD, and ACOX1 in the heart of rats[4].

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

    471.49

    Formula

    C21H17F4NO3S2
    CAS 號
    性狀

    固體

    顏色

    White to light yellow

    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 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : ≥ 34 mg/mL (72.11 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 2.1209 mL 10.6047 mL 21.2094 mL
    5 mM 0.4242 mL 2.1209 mL 4.2419 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, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

    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 (5.30 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 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.30 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，此方案實(shí)驗(yàn)周期在半個月以上的動物實(shí)驗(yàn)酌情使用。

      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玉米油中，混合均勻。

    動物溶解方案計算器
    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: 99.94%

    參考文獻(xiàn)
    Cell Assay
    [2]

    The PPARβ activator GW0742 and the RXR activator 9-cis-retinoic acid are dissolved in DMSO. The final DMSO concentration des not exceed 0.5% v/v, and this concentration is used in control wells. For each culture plate, one row of wells is treated with 500 μM glutamate. These wells serve as a positive control and for normalisation of data. Cell death (toxicity) is assessed by using an assay designed to measure lactate dehydrogenase (LDH) release[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Male CD mice (25-35 g) are housed in a controlled environment and provided with standard rodent chow and water. Mice are randomized into four experimental groups: bleomycin-treated group: mice are subjected to lung injury induced by intratracheal instillation of bleomycin and treated daily via intraperitoneal injection with vehicle of GW0742 (10% dimethylsulfoxide (OMSO, 1 mL/kg), 1 h after BLEO instillation (n = 15). GW0742 group: identical to bleomycin-treated group but mice are treated daily with GW0742 (0.3 mg/kg, 1h after BLEO instillation) via intraperitoneal injection (n = 15). Sham-operated mice + vehicle group: animals are subjected to the identical surgical procedure but receive intratracheal instillation of saline (0.9%) instead of BLEO and are treated daily with the vehicle of GW0742 (10% dimethylsulfoxide (DMSO), 1 mL/kg, i.p.), 1 h after saline instillation (n = 15). Sham-operated mice + GW0742 group: identical to sham + vehicle group but mice are treated daily with GW0742 (0.3 mg/kg, 1 h after saline instillation) via intraperitoneal injection (n = 15)[3].

    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, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(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 2.1209 mL 10.6047 mL 21.2094 mL 53.0234 mL
    5 mM 0.4242 mL 2.1209 mL 4.2419 mL 10.6047 mL
    10 mM 0.2121 mL 1.0605 mL 2.1209 mL 5.3023 mL
    15 mM 0.1414 mL 0.7070 mL 1.4140 mL 3.5349 mL
    20 mM 0.1060 mL 0.5302 mL 1.0605 mL 2.6512 mL
    25 mM 0.0848 mL 0.4242 mL 0.8484 mL 2.1209 mL
    30 mM 0.0707 mL 0.3535 mL 0.7070 mL 1.7674 mL
    40 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3256 mL
    50 mM 0.0424 mL 0.2121 mL 0.4242 mL 1.0605 mL
    60 mM 0.0353 mL 0.1767 mL 0.3535 mL 0.8837 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.

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    產(chǎn)品名稱：
    GW0742
    目錄號：
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