GW0742
Based on 18 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.64%
- No. CAS: 317318-84-6
- Fòrmula: C21H17F4NO3S2
- Peso molecular:471.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) GW0742
More- Cell Death Dis. 2024 Aug 26;15(8):623. [Abstract]
- Pharmacol Res. 2020 Mar;153:104679. [Abstract]
- Biol Psychiatry. 2021 Mar 15;89(6):615-626. [Abstract]
- Environ Res. 2025 Oct 17:287:123154. [Abstract]
- Brain Behav Immun. 2024 Jul:119:56-83. [Abstract]
- Br J Pharmacol. 2020 May;177(10):2286-2302. [Abstract]
- Eur J Med Chem. 2022 Feb 5:229:114061. [Abstract]
- Eur J Med Chem. 2021 Dec 5:225:113807. [Abstract]
- Liver Int. 2023 Dec;43(12):2808-2823. [Abstract]
- Cells. 2025 Nov 22;14(23):1843. [Abstract]
- Eur J Pharmacol. 2020 Sep 5;882:173300. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2018 Oct;1864(10):3322-3338. [Abstract]
- Biosci Rep. 2020 May 29;40(5):BSR20200559. [Abstract]
- Toxicol Appl Pharmacol. 2025 Jan:494:117180. [Abstract]
- Bioorg Med Chem. 2022 Feb 15:56:116615. [Abstract]
- J Pharm Biomed Anal. 2021 Feb 20:195:113870. [Abstract]
- PPAR Res. 2020 Dec 22:2020:8864813. [Abstract]
- bioRxiv. 2025 Nov 30:2025.10.02.680018. [Abstract]
Customer Validation & Images
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In Vivo Imaging
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RT-PCR
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IF
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
Actividad biológica
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PPARδ 1 nM (EC50) |
PPARα 1.1 μM (EC50) |
PPARγ 2 μM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
≤5.8 nM
Compound: GW-0742
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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
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[PMID: 21074432] |
| HEK293 | EC50 |
13 nM
Compound: GW0742
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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
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[PMID: 30605833] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 317318-84-6
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Appearance Solid
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Peso molecular 471.49
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Fòrmula C21H17F4NO3S2
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Color White to light yellow
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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
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Synonyms
GW610742
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (18)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
TREM2-dependent activation of microglial cell protects photoreceptor cell during retinal degeneration via PPARγ and CD36. [Abstract]2024 Aug 26;15(8):623. PMID: 39187498
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.
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Pharmacol Res
A novel FFA1 agonist, CPU025, improves glucose-lipid metabolism and alleviates fatty liver in obese-diabetic (ob/ob) mice. [Abstract]2020 Mar;153:104679. PMID: 32014571 -
Biol Psychiatry
Transcription Factor TWIST1 Integrates Dendritic Remodeling and Chronic Stress to Promote Depressive-like Behaviors. [Abstract]2021 Mar 15;89(6):615-626. PMID: 33190845
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).
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Environ Res
Prenatal exposure to environmental metal mixtures and social development in early childhood: Evidence from a birth cohort and mechanistic study. [Abstract]2025 Oct 17:287:123154. PMID: 41110787
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.
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Brain Behav Immun
2024 Jul:119:56-83. PMID: 38555992
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.
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Br J Pharmacol
HWL-088, a new potent free fatty acid receptor 1 (FFAR1) agonist, improves glucolipid metabolism and acts additively with metformin in ob/ob diabetic mice. [Abstract]2020 May;177(10):2286-2302. PMID: 31971610 -
Eur J Med Chem
Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents. [Abstract]2022 Feb 5:229:114061. PMID: 34954593 -
Eur J Med Chem
Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome. [Abstract]2021 Dec 5:225:113807. PMID: 34455359 -
Liver Int
2023 Dec;43(12):2808-2823. PMID: 37833850 -
Cells
The Role of PPARβ/δ-Related Lipid Metabolism in High-Altitude Adaptation of Yak Coat Based on Proteomics and Metabolomics. [Abstract]2025 Nov 22;14(23):1843. PMID: 41369331 -
Eur J Pharmacol
Hepatoprotective effects of ZLY16, a dual peroxisome proliferator-activated receptor α/δ agonist, in rodent model of nonalcoholic steatohepatitis. [Abstract]2020 Sep 5;882:173300. PMID: 32592770 -
Biochim Biophys Acta Mol Basis Dis
LAZ3 protects cardiac remodeling in diabetic cardiomyopathy via regulating miR-21/PPARa signaling. [Abstract]2018 Oct;1864(10):3322-3338. PMID: 30031228
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.
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Biosci Rep
VCAM-1-targeted and PPARδ-agonist-loaded nanomicelles enhanced suppressing effects on apoptosis and migration of oxidized low-density lipoprotein-induced vascular smooth muscle cells. [Abstract]2020 May 29;40(5):BSR20200559. PMID: 32314783 -
Toxicol Appl Pharmacol
PPARβ/δ agonist GW0742 mitigates acute liver damage induced by acetaminophen overdose in mice. [Abstract]2025 Jan:494:117180. PMID: 39617257 -
Bioorg Med Chem
Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold. [Abstract]2022 Feb 15:56:116615. PMID: 35051813 -
J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569 -
PPAR Res
Ligand-Activated Peroxisome Proliferator-Activated Receptor β/ δ Facilitates Cell Proliferation in Human Cholesteatoma Keratinocytes. [Abstract]2020 Dec 22:2020:8864813. PMID: 33424958 -
bioRxiv
A Micro-Engineered Heart Tissue Model of Desmin-related Cardiomyopathy Caused by Mutant αB Crystallin. [Abstract]2025 Nov 30:2025.10.02.680018. PMID: 41256615
Solvente y solubilidad
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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) has not independently confirmed the accuracy of these methods. They are for reference only.
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) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Sznaidman ML, et al. Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity. Bioorg Med Chem Lett. 2003 May 5;13(9):1517-21. [Content Brief]
[2]. Smith SA, et al. Effect of the peroxisome proliferator-activated receptor beta activator GW0742 in rat cultured cerebellar granule neurons. J Neurosci Res. 2004 Jul 15;77(2):240-9. [Content Brief]
[3]. Galuppo M, et al. GW0742, a high affinity PPAR-β/δ agonist reduces lung inflammation induced by bleomycin instillation in mice. Int J Immunopathol Pharmacol. 2010 Oct-Dec;23(4):1033-46. [Content Brief]
[4]. Kuo SC, et al. Activation of receptors δ (PPARδ) by agonist (GW0742) may enhance lipid metabolism in heart both in vivo and in vitro. Horm Metab Res. 2013 Nov;45(12):880-6. [Content Brief]
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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