Art. -Nr.: HY-13928

GW0742

(Synonyms: GW610742)

18 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.64%
CAS. Nr.: 317318-84-6
Formel: C₂₁H₁₇F₄NO₃S₂
Molecular Weight:471.49

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GW0742 Chemical Structure

CAS. Nr.: 317318-84-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (18)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PPARδ

1 nM (EC₅₀)

PPARα

1.1 μM (EC₅₀)

PPARγ

2 μM (EC₅₀)

Alle PPAR Isoform-spezifische Produkte anzeigen :

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]

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].

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

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].

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

Chemical Information

CAS. Nr. 317318-84-6
Appearance Solid
Molecular Weight 471.49
Formel C₂₁H₁₇F₄NO₃S₂
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
Synonyms

GW610742
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (18)

All Bio/Physico-chemical AssayIn Vivo ImagingIn Vivo Efficacy StudyRT-PCRCell Imaging/StainingWBIF

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Journal Impact Factor

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.
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).
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.
Brain Behav Immun

A TrkB cleavage fragment in hippocampus promotes Depressive-Like behavior in mice. [Abstract]

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.
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

PPARβ/δ activation protects against hepatic ischaemia-reperfusion injury. [Abstract]

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.
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

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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].

MedChemExpress (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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

GW0742

18 Cited Publications

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GW0742

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

Pyroptosis Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Lipid Metabolism Compound Library

Antidepressant Compound Library

Human Metabolite Library

Nuclear Receptor Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) GW0742

Alle PPAR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (18)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GW0742

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

Pyroptosis Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Lipid Metabolism Compound Library

Antidepressant Compound Library

Human Metabolite Library

Nuclear Receptor Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) GW0742

Alle PPAR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (18)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GW0742 Related Classifications

HY-13928 Related Classifications