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

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.

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CAS 番号 : 317318-84-6

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 57 在庫あり
Solution
10 mM * 1 mL in DMSO USD 57 在庫あり
Solid
5 mg $55 在庫あり
10 mg $88 在庫あり
25 mg $190 在庫あり
50 mg $308 在庫あり
100 mg $539 在庫あり
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カスタマーレビュー

Based on 18 publication(s) in Google Scholar

Other Forms of GW0742:

GW0742 関連抗体

Top Publications Citing Use of Products

    GW0742 purchased from MedChemExpress. Usage Cited in: Environ Res. 2025 Oct 17:287:123154.  [Abstract]

    GW0742 (20 μM; 0 to 120 hpf (approximately 1 h post-fertilization)) significantly ameliorated the motor impairments induced by Mix N exposure, as evidenced by an increase in distance moved during light/dark cycles. Subsequent social preference assays on day 21 confirmed that activation of the PPAR signaling pathway improved the social capabilities of zebrafish larvae, as indicated by increased locomotor activity, travel distance, and duration spent in the targeted zone compared to the Mix N-exposed group.

    GW0742 purchased from MedChemExpress. Usage Cited in: Environ Res. 2025 Oct 17:287:123154.  [Abstract]

    GW0742 (20 μM; 0 to 120 hpf (approximately 1 h post-fertilization)) significantly mitigated blood-brain barrier disruption caused by Mix N exposure, resulting in a marked reduction in the expression of BBB-related genes in Zebrafish larvae.

    GW0742 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Aug 26;15(8):623.  [Abstract]

    GW0742 (20 mg/kg; IP; twice) in WT and Trem2−/− mice showed no significant changes in the number of microglial cells migrating towards the ONL.(A) Representative immunofluorescent images of IBA1-stained cells following GW0742 treatment in Trem2-/- and WT mice at 3 days post-MNU treatment.(B) Comparison of the infiltration and distribution of IBA1+ cells between WT and Trem2-/- mouse retina at 3 days post-MNU treatment and PPARβ/δ agonist treatment.

    GW0742 purchased from MedChemExpress. Usage Cited in: Brain Behav Immun. 2024 Jul:119:56-83.  [Abstract]

    Primary neurons were firstly infected with rAAV-GFP or rAAV-TrkB 1–486 at DIV 3, and subsequently treated with vehicle or GW0742 (1 mM) at DIV 6 for 48 h. Measurement of MMP and ATP levels in primary hippocampal neurons with indicated treatments.

    GW0742 purchased from MedChemExpress. Usage Cited in: Brain Behav Immun. 2024 Jul:119:56-83.  [Abstract]

    GW0742 (1 mM; 48 h) could reverse the impaired dendritic morphogenesis. Representative immunofluorescence images of GFP (green) labeling in primary hippocampal neurons of mice treated with indicative treatments.

    GW0742 purchased from MedChemExpress. Usage Cited in: Biol Psychiatry. 2021 Mar 15;89(6):615-626.  [Abstract]

    GW0742 (1 μM) rescued AAVTWIST1 treatment reduced MMP in neurons. Quantification of mitochondrial membrane potential in primary cultured cortical neurons transfected with AAV-TWIST1 or AAV-Flag. CCCP treatment served as a positive control for depolarization.

    GW0742 purchased from MedChemExpress. Usage Cited in: Biol Psychiatry. 2021 Mar 15;89(6):615-626.  [Abstract]

    GW0742 (50 μM; intra-mPFC injection once daily for 7 days) rescued depressive-like behaviors induced by chronic social defeat stress (CSDS).

    GW0742 purchased from MedChemExpress. 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.

    PPAR アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PPARα PPARβ/δ PPARγ PPAR PPARδ

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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)

    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]
    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]
    体外実験

    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].

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

    GW0742 関連抗体
    体内実験

    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].

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

    471.49

    分子式

    C21H17F4NO3S2
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(O)COC1=CC=C(SCC2=C(C)N=C(C3=CC=C(C(F)(F)F)C(F)=C3)S2)C=C1C
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 34 mg/mL (72.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.2121 mL 1.0605 mL 2.1209 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

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    体積 （開始）

    V1

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    濃度 （終了）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
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    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション
    参考文献
    細胞実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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
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    GW0742 Related Classifications

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    GW0742317318-84-6GW610742GW 0742GW-0742GW 610742GW-610742PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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    製品名:
    GW0742
    製品番号:
    HY-13928
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