GW-0742
GW-0742 activates PPAR-beta/delta and changes metabolism in cells and animals. In the commonly cited trained-mouse experiment, GW-0742 alone did not significantly improve running time; the large endurance result belonged to its combination with AICAR. The cited evidence contains no human efficacy or pharmacokinetic study.
experimental PPAR-beta/delta agonist
- Also called GW0742, GW610742, and Fitorine
- Distinct from GW501516/Cardarine; classified as a PPAR-delta agonist
- No cited human administration or human pharmacokinetic study
- WADA's PPAR-delta-agonist class prohibition applies in 2026
Is GW-0742 just another name for Cardarine or GW501516?
GW-0742 and GW501516 are separate compounds. Both can activate PPAR-beta/delta, but their toxicology, pharmacokinetics, and clinical evidence are not interchangeable.
PubChem · GW-0742 identity
Official chemical identity record
National Center for Biotechnology Information. PubChem CID 9934458.
The record identifies GW0742 with formula C21H17F4NO3S2, molecular weight 471.5 g/mol, CAS 317318-84-6, and UNII 4PZK9FJC4Z. This differs from GW501516's identity and CAS.
- Study design
- Chemical database record
Identity is not approval or product authentication.
Read the original sourceSznaidman et al. · GW0742 discovery
Medicinal-chemistry and cell pharmacology study
Sznaidman ML, Haffner CD, Maloney PR, Fivush A, Chao E, Goreham D, Sierra ML, LeGrumelec C, Xu HE, Montana VG, Lambert MH, Willson TM, Oliver WR, Sternbach DD. Bioorganic & Medicinal Chemistry Letters. 2003;13(9):1517-1521. DOI 10.1016/S0960-894X(03)00207-5.
The discovery series identified the distinct compounds GW501516 and GW0742; GW0742 showed low-nanomolar PPAR-delta agonism with strong selectivity over human PPAR-alpha and PPAR-gamma in the reported assays.
- Participants / model
- Receptor and cell assay systems
- Treatment
- Medicinal-chemistry series including GW501516 and GW0742
- Study design
- Compound synthesis and in-vitro pharmacology
- Funding
- GlaxoSmithKline-associated discovery work
The assay measured receptor potency and selectivity. It included no human efficacy or safety outcome.
Read the original sourceWhat does GW-0742 do?
GW-0742 binds and activates the PPAR-beta/delta nuclear receptor, changing transcription involved in lipid handling, energy metabolism, inflammation, and other tissue-specific programs. It was designed with strong selectivity over PPAR-alpha and PPAR-gamma at low concentrations, but high-concentration cell assays found broader nuclear-receptor antagonism.
Target selectivity is concentration- and assay-dependent. The molecule's original low-concentration PPAR profile and its high-micromolar off-target behavior can both be true.
Sznaidman et al. · GW0742 discovery
Medicinal-chemistry and cell pharmacology study
Sznaidman ML, Haffner CD, Maloney PR, Fivush A, Chao E, Goreham D, Sierra ML, LeGrumelec C, Xu HE, Montana VG, Lambert MH, Willson TM, Oliver WR, Sternbach DD. Bioorganic & Medicinal Chemistry Letters. 2003;13(9):1517-1521. DOI 10.1016/S0960-894X(03)00207-5.
The discovery series identified the distinct compounds GW501516 and GW0742; GW0742 showed low-nanomolar PPAR-delta agonism with strong selectivity over human PPAR-alpha and PPAR-gamma in the reported assays.
- Participants / model
- Receptor and cell assay systems
- Treatment
- Medicinal-chemistry series including GW501516 and GW0742
- Study design
- Compound synthesis and in-vitro pharmacology
- Funding
- GlaxoSmithKline-associated discovery work
The assay measured receptor potency and selectivity. It included no human efficacy or safety outcome.
Read the original sourceNandhikonda et al. · high-concentration off-targets
Cell and biochemical receptor study
Nandhikonda P, Yasgar A, Baranowski AM, Sidhu PS, McCallum MM, Pawlak AJ, Teske K, Feleke B, Yuan NY, Kevin C, Bikle DD, Ayers SD, Webb P, Rai G, Simeonov A, Jadhav A, Maloney D, Arnold LA. Biochemistry. 2013. DOI 10.1021/bi400321p.
GW0742 weakly interacted with multiple nuclear receptors and became a broad nuclear-receptor antagonist above 12.1 micromolar in the reported cell and biochemical assays, with notable activity at vitamin D and androgen receptor systems.
- Participants / model
- Biochemical and cell receptor assays
- Treatment
- GW0742 across assay concentrations
- Study design
- High-throughput follow-up and receptor profiling
These receptor assays used cell concentrations; they do not establish an in vivo human interaction threshold.
Read the original sourceDoes GW-0742 itself improve endurance?
The cited trained-mouse experiment did not find a significant running-time benefit from GW-0742 alone. Only the AICAR plus GW-0742 combination significantly beat trained vehicle on time to exhaustion.
Five groups separated sedentary vehicle, trained vehicle, GW-0742, AICAR and the combination. Endpoint groups contained seven or eight male mice after four weeks. AICAR increased calculated work, and the combination exceeded it. The quoted 138 to 179% endurance advantage belongs to combination comparisons.
GW-0742 changes oxidative-pathway markers in muscle, but those changes do not demonstrate human endurance or fat loss. The cited evidence contains no human concentration-time or performance dataset.
Combined AMPK/PPAR-delta activation in trained mice
Primary preclinical study
Manio MC, Inoue K, Fujitani M, Matsumura S, Fushiki T. Combined pharmacological activation of AMPK and PPARδ potentiates the effects of exercise in trained mice. Physiological reports. 2016. DOI 10.14814/phy2.12625.
Five groups separated sedentary vehicle, trained vehicle, GW0742, AICAR and combination. Endpoint groups were 7 to 8 male BALB/c mice. After four weeks, only the combination significantly increased time to exhaustion over trained vehicle; AICAR improved calculated work, and combination exceeded it. GW0742 alone did not significantly improve running time. The large quoted 138 to 179% advantage belongs to combination comparisons, not GW0742 monotherapy. Multiple endpoints, forced treadmill testing and small groups limit translation.
- Participants / model
- Seven-week-old male BALB/c mice
- Treatment
- Exercise plus vehicle, injected GW0742, injected AICAR, or both
- Follow-up
- 4 weeks
- Study design
- Controlled animal combination and exercise study
PPAR-beta activation and AMPK subunits in muscle
Primary preclinical study
Lendoye E, Sibille B, Rousseau AS, Murdaca J, Grimaldi PA, Lopez P. PPARbeta activation induces rapid changes of both AMPK subunit expression and AMPK activation in mouse skeletal muscle. Molecular endocrinology (Baltimore, Md.). 2011. DOI 10.1210/me.2010-0504.
GW0742 rapidly changed AMPK subunit expression in mouse muscle and cultured myotubes. This provides a mechanistic link to oxidative remodeling, not a measured human performance outcome. A protein-expression response cannot be graded as endurance efficacy.
Read the original sourceHuman evidence · no clinical performance result
PubMed and ClinicalTrials.gov records
PubMed and ClinicalTrials.gov records for GW0742 human administration and performance.
The cited records include no human administration, exercise, endurance, body-composition, or pharmacokinetic study. Human-cell studies do not constitute human clinical evidence.
- Participants / model
- Published and registered GW0742 records
What did the Russian GW-0742 epilepsy program find?
A 2024 Russian Academy of Sciences team gave GW-0742 to male Wistar rats in a lithium-pilocarpine temporal-lobe-epilepsy model for seven days. The paper reported partial changes in selected behavioral and glial endpoints. It did not test seizure prevention, people, or performance.
The Russian-language conference abstracts and proceedings describe rat experiments from the same Saint Petersburg group as the peer-reviewed English paper, so they are not independent replication.
| Record | Publication format | Evidence |
|---|---|---|
| International Journal of Molecular Sciences paper | Peer-reviewed English paper; Russian authors and institution | Four rat groups; seven-day GW-0742 exposure; behavior plus brain mRNA and protein endpoints |
| Биохимия человека proceedings | Russian conference proceedings | Overlapping male-Wistar lithium-pilocarpine model and glial-expression endpoints; group size and exposure detail incomplete in abstract |
| Saint Petersburg conference records | Russian conference abstract and program | Additional descriptions of the same research line; not a human or performance study |
Russian GW0742/Fitorine rat epilepsy program, 2024
Primary preclinical study
Zubareva OE, Kharisova AR, Roginskaya AI, Kovalenko AA, Zakharova MV, Schwarz AP, Sinyak DS, Zaitsev AV. PPARβ/δ Agonist GW0742 Modulates Microglial and Astroglial Gene Expression in a Rat Model of Temporal Lobe Epilepsy. International journal of molecular sciences. 2024. DOI 10.3390/ijms251810015.
Seven-day treatment after lithium-pilocarpine injury partly altered behavior and astroglial/microglial expression. Behavioral groups were roughly 8 to 12 rats, with smaller endpoint-specific samples. The associated Russian proceedings describe the same research program and are not independent clinical replication.
- Participants / model
- Male Wistar rats, control and lithium-pilocarpine temporal-lobe-epilepsy groups
- Treatment
- GW0742/Fitorine 5 mg/kg/day for seven days versus vehicle
- Follow-up
- 7 days with subsequent behavior and tissue endpoints
- Study design
- Controlled four-group animal study
- Funding
- Russian Science Foundation project 23-25-00480
Kharisova et al. · Russian conference abstract
Preclinical rat study, Russian-language conference proceedings abstract
Харисова А.Р., Рогинская А.И., Захарова М.В., Шварц А.П., Зубарева О.Е. Биохимия человека: материалы всероссийской конференции с международным участием. 2024:78-79.
The Russian abstract describes male Wistar rats aged seven to eight weeks in a lithium-pilocarpine temporal-lobe-epilepsy model. Early GW0742 treatment altered selected glial activation and inflammatory-gene markers in hippocampus and temporal cortex.
- Participants / model
- Male Wistar rats aged 7 to 8 weeks
- Treatment
- Course of GW0742 during the first week after model induction
- Follow-up
- First week; latent-phase evaluation
- Study design
- Conference-abstract report of controlled animal work
- Funding
- Russian Science Foundation project 23-25-00480
The Russian-language proceedings overlap the later full paper and are not independent replication. The abstract does not report group size or GW0742 exposure.
Read the original sourceChinese and Russian records · rat programs
Preclinical literature
Chinese and Russian literature and registry records for GW0742.
The cited Chinese record describes a China-affiliated acetaminophen acute-liver-injury mouse study. The cited Russian records describe the Saint Petersburg rat epilepsy program, including Russian proceedings and a peer-reviewed English paper. These sources include no human administration or pharmacokinetic result.
- Participants / model
- Chinese- and Russian-language literature and registry records
The Russian conference and index records overlap the peer-reviewed English paper and are not independent evidence. The Chinese registry record does not provide enough study detail to evaluate.
Read the original sourceWhat compound-specific harm has been documented?
A 10-day mouse toxicology paper found marked liver injury and degenerative skeletal myopathy at high GW-0742 exposures, especially in wild-type mice; PPAR-alpha-null animals were less affected. A later acetaminophen-injury model reported liver protection at a different exposure and disease context.
These results are context-dependent. The toxicology paper tested otherwise healthy mice at high exposures. The China-affiliated paper tested prevention or treatment of an induced acute liver injury and remains abstract-level. Neither supplies a human event rate or threshold.
High-exposure GW0742 liver and muscle toxicology
Primary preclinical study
Faiola B, Falls JG, Peterson RA, Bordelon NR, Brodie TA, Cummings CA, Romach EH, Miller RT. PPAR alpha, more than PPAR delta, mediates the hepatic and skeletal muscle alterations induced by the PPAR agonist GW0742. Toxicological sciences : an official journal of the Society of Toxicology. 2008. DOI 10.1093/toxsci/kfn130.
Ten-day controlled wild-type/PPAR-alpha-null mouse experiments found marked liver and muscle abnormalities at the highest exposure, with attenuated injury in knockout mice. This is compound-specific hazard evidence. The experimental exposures do not establish a human event rate, safe threshold or equivalence to chronic GW501516 carcinogenicity.
- Participants / model
- Male wild-type and PPAR-alpha-null mice; ten per genotype and treatment condition
- Treatment
- GW0742 and a PPAR-alpha comparator at toxicological exposures
- Follow-up
- 10 days
- Study design
- Controlled knockout-mechanism toxicology study
- Funding
- Industry-associated toxicology program
Nandhikonda et al. · high-concentration off-targets
Cell and biochemical receptor study
Nandhikonda P, Yasgar A, Baranowski AM, Sidhu PS, McCallum MM, Pawlak AJ, Teske K, Feleke B, Yuan NY, Kevin C, Bikle DD, Ayers SD, Webb P, Rai G, Simeonov A, Jadhav A, Maloney D, Arnold LA. Biochemistry. 2013. DOI 10.1021/bi400321p.
GW0742 weakly interacted with multiple nuclear receptors and became a broad nuclear-receptor antagonist above 12.1 micromolar in the reported cell and biochemical assays, with notable activity at vitamin D and androgen receptor systems.
- Participants / model
- Biochemical and cell receptor assays
- Treatment
- GW0742 across assay concentrations
- Study design
- High-throughput follow-up and receptor profiling
These receptor assays used cell concentrations; they do not establish an in vivo human interaction threshold.
Read the original sourceChinese acetaminophen liver-injury study, 2024
Primary preclinical study
Wang L, Chen JH, Zhang YJ, Zhang MB, Zeng T. PPARβ/δ agonist GW0742 mitigates acute liver damage induced by acetaminophen overdose in mice. Toxicology and applied pharmacology. 2025. DOI 10.1016/j.taap.2024.117180.
Preventive and delayed GW0742 treatment improved selected biochemical and histological injury measures in mice, including treatment six hours after acetaminophen. This supports a disease-model hypothesis. It cannot be used to claim GW0742 is nonhepatotoxic in healthy users.
- Participants / model
- Male mice in an acetaminophen acute-liver-injury model
- Treatment
- Intraperitoneal GW0742 before or after acetaminophen, with vehicle and N-acetylcysteine comparisons
- Follow-up
- Acute injury experiment
- Study design
- Controlled preclinical disease-model study
Is there a human half-life, safe threshold, or interaction guide?
The cited ClinicalTrials.gov and PubMed records include no human administration study or concentration-time dataset. Rat, mouse, cell, or reagent-vendor numbers cannot supply human half-life, oral bioavailability, dosing frequency, contraindications, interactions, or a safe threshold.
ClinicalTrials.gov · no GW0742 study listed
Clinical trial registry
ClinicalTrials.gov records for GW0742, GW-0742, GW610742, and Fitorine.
ClinicalTrials.gov lists no study under GW0742, GW-0742, GW610742, or Fitorine. The cited public evidence also includes no human administration or concentration-time paper.
- Participants / model
- ClinicalTrials.gov records
- Treatment
- GW0742
Chinese and Russian records · rat programs
Preclinical literature
Chinese and Russian literature and registry records for GW0742.
The cited Chinese record describes a China-affiliated acetaminophen acute-liver-injury mouse study. The cited Russian records describe the Saint Petersburg rat epilepsy program, including Russian proceedings and a peer-reviewed English paper. These sources include no human administration or pharmacokinetic result.
- Participants / model
- Chinese- and Russian-language literature and registry records
The Russian conference and index records overlap the peer-reviewed English paper and are not independent evidence. The Chinese registry record does not provide enough study detail to evaluate.
Read the original sourceIs GW-0742 approved or allowed in tested sport?
The cited regulatory and clinical records show no approved medicine or human clinical program. WADA's 2026 S4.4.1 section prohibits PPAR-delta agonists at all times using an including-but-not-limited-to list. GW-0742 is not named individually; the class placement follows its primary pharmacology.
WADA 2026 · PPAR-delta-agonist class applies
Official anti-doping standard
World Anti-Doping Agency. The 2026 Prohibited List, effective 1 January 2026.
Section S4.4.1 prohibits PPAR-delta agonists at all times using an including-but-not-limited-to list. It names GW1516/GW501516 as an example but does not name GW0742.
- Participants / model
- Athletes subject to the World Anti-Doping Code
- Follow-up
- Calendar year 2026
- Study design
- Anti-doping prohibited list
- Funding
- World Anti-Doping Agency
GW0742 class placement follows its primary PPAR-delta pharmacology; the named Cardarine example is a different molecule.
Read the original sourceSznaidman et al. · GW0742 discovery
Medicinal-chemistry and cell pharmacology study
Sznaidman ML, Haffner CD, Maloney PR, Fivush A, Chao E, Goreham D, Sierra ML, LeGrumelec C, Xu HE, Montana VG, Lambert MH, Willson TM, Oliver WR, Sternbach DD. Bioorganic & Medicinal Chemistry Letters. 2003;13(9):1517-1521. DOI 10.1016/S0960-894X(03)00207-5.
The discovery series identified the distinct compounds GW501516 and GW0742; GW0742 showed low-nanomolar PPAR-delta agonism with strong selectivity over human PPAR-alpha and PPAR-gamma in the reported assays.
- Participants / model
- Receptor and cell assay systems
- Treatment
- Medicinal-chemistry series including GW501516 and GW0742
- Study design
- Compound synthesis and in-vitro pharmacology
- Funding
- GlaxoSmithKline-associated discovery work
The assay measured receptor potency and selectivity. It included no human efficacy or safety outcome.
Read the original sourceClinicalTrials.gov · no GW0742 study listed
Clinical trial registry
ClinicalTrials.gov records for GW0742, GW-0742, GW610742, and Fitorine.
ClinicalTrials.gov lists no study under GW0742, GW-0742, GW610742, or Fitorine. The cited public evidence also includes no human administration or concentration-time paper.
- Participants / model
- ClinicalTrials.gov records
- Treatment
- GW0742
What do the Chinese- and Russian-language records add?
A Saint Petersburg group reported a rat epilepsy program, and a Shandong University abstract reported an acetaminophen liver-injury mouse model. Neither involved human administration or human pharmacokinetics.
Chinese and Russian records · rat programs
Preclinical literature
Chinese and Russian literature and registry records for GW0742.
The cited Chinese record describes a China-affiliated acetaminophen acute-liver-injury mouse study. The cited Russian records describe the Saint Petersburg rat epilepsy program, including Russian proceedings and a peer-reviewed English paper. These sources include no human administration or pharmacokinetic result.
- Participants / model
- Chinese- and Russian-language literature and registry records
The Russian conference and index records overlap the peer-reviewed English paper and are not independent evidence. The Chinese registry record does not provide enough study detail to evaluate.
Read the original sourceRussian GW0742/Fitorine rat epilepsy program, 2024
Primary preclinical study
Zubareva OE, Kharisova AR, Roginskaya AI, Kovalenko AA, Zakharova MV, Schwarz AP, Sinyak DS, Zaitsev AV. PPARβ/δ Agonist GW0742 Modulates Microglial and Astroglial Gene Expression in a Rat Model of Temporal Lobe Epilepsy. International journal of molecular sciences. 2024. DOI 10.3390/ijms251810015.
Seven-day treatment after lithium-pilocarpine injury partly altered behavior and astroglial/microglial expression. Behavioral groups were roughly 8 to 12 rats, with smaller endpoint-specific samples. The associated Russian proceedings describe the same research program and are not independent clinical replication.
- Participants / model
- Male Wistar rats, control and lithium-pilocarpine temporal-lobe-epilepsy groups
- Treatment
- GW0742/Fitorine 5 mg/kg/day for seven days versus vehicle
- Follow-up
- 7 days with subsequent behavior and tissue endpoints
- Study design
- Controlled four-group animal study
- Funding
- Russian Science Foundation project 23-25-00480
Chinese acetaminophen liver-injury study, 2024
Primary preclinical study
Wang L, Chen JH, Zhang YJ, Zhang MB, Zeng T. PPARβ/δ agonist GW0742 mitigates acute liver damage induced by acetaminophen overdose in mice. Toxicology and applied pharmacology. 2025. DOI 10.1016/j.taap.2024.117180.
Preventive and delayed GW0742 treatment improved selected biochemical and histological injury measures in mice, including treatment six hours after acetaminophen. This supports a disease-model hypothesis. It cannot be used to claim GW0742 is nonhepatotoxic in healthy users.
- Participants / model
- Male mice in an acetaminophen acute-liver-injury model
- Treatment
- Intraperitoneal GW0742 before or after acetaminophen, with vehicle and N-acetylcysteine comparisons
- Follow-up
- Acute injury experiment
- Study design
- Controlled preclinical disease-model study
What else does PPAR-delta activation change?
The effects extend beyond muscle. Human T-cell cultures and trained mice showed changes in fuel use and immune-cell composition, without a demonstrated clinical immune benefit or harm.
A 2021 experiment exposed human T cells in vitro and used six mice per group for its chronic treatment experiment. Fatty-acid-oxidation potential increased, and treatment plus exercise changed lymph-node regulatory T-cell proportions. People did not receive GW-0742 in that experiment.
PPAR-delta agonism, training and T-cell metabolism, 2021
Primary preclinical study
Sibille B, Mothe-Satney I, Le Menn G, Lepouse D, Le Garf S, Baudoin E, Murdaca J, Moratal C, Lamghari N, Chinetti G, Neels JG, Rousseau AS. Gene Doping with Peroxisome-Proliferator-Activated Receptor Beta/Delta Agonists Alters Immunity but Exercise Training Mitigates the Detection of Effects in Blood Samples. International journal of molecular sciences. 2021. DOI 10.3390/ijms222111497.
Human T cells were exposed in vitro; mice received six weeks of dietary GW0742 during an eight-week exercise program, with six animals per treatment group for the chronic experiment. Fatty-acid-oxidation potential increased, and combined treatment/training altered lymph-node Treg proportions. Blood signatures were partly masked by training. This expands mechanism and raises immunological questions; it did not demonstrate clinically important infection or immune harm in humans. The paper’s internet-dose discussion is not validated human PK.
Read the original sourceStudies and sources
PubChem · GW-0742 identity
Official chemical identity record
National Center for Biotechnology Information. PubChem CID 9934458.
The record identifies GW0742 with formula C21H17F4NO3S2, molecular weight 471.5 g/mol, CAS 317318-84-6, and UNII 4PZK9FJC4Z. This differs from GW501516's identity and CAS.
- Study design
- Chemical database record
Identity is not approval or product authentication.
Read the original sourceSznaidman et al. · GW0742 discovery
Medicinal-chemistry and cell pharmacology study
Sznaidman ML, Haffner CD, Maloney PR, Fivush A, Chao E, Goreham D, Sierra ML, LeGrumelec C, Xu HE, Montana VG, Lambert MH, Willson TM, Oliver WR, Sternbach DD. Bioorganic & Medicinal Chemistry Letters. 2003;13(9):1517-1521. DOI 10.1016/S0960-894X(03)00207-5.
The discovery series identified the distinct compounds GW501516 and GW0742; GW0742 showed low-nanomolar PPAR-delta agonism with strong selectivity over human PPAR-alpha and PPAR-gamma in the reported assays.
- Participants / model
- Receptor and cell assay systems
- Treatment
- Medicinal-chemistry series including GW501516 and GW0742
- Study design
- Compound synthesis and in-vitro pharmacology
- Funding
- GlaxoSmithKline-associated discovery work
The assay measured receptor potency and selectivity. It included no human efficacy or safety outcome.
Read the original sourceCombined AMPK/PPAR-delta activation in trained mice
Primary preclinical study
Manio MC, Inoue K, Fujitani M, Matsumura S, Fushiki T. Combined pharmacological activation of AMPK and PPARδ potentiates the effects of exercise in trained mice. Physiological reports. 2016. DOI 10.14814/phy2.12625.
Five groups separated sedentary vehicle, trained vehicle, GW0742, AICAR and combination. Endpoint groups were 7 to 8 male BALB/c mice. After four weeks, only the combination significantly increased time to exhaustion over trained vehicle; AICAR improved calculated work, and combination exceeded it. GW0742 alone did not significantly improve running time. The large quoted 138 to 179% advantage belongs to combination comparisons, not GW0742 monotherapy. Multiple endpoints, forced treadmill testing and small groups limit translation.
- Participants / model
- Seven-week-old male BALB/c mice
- Treatment
- Exercise plus vehicle, injected GW0742, injected AICAR, or both
- Follow-up
- 4 weeks
- Study design
- Controlled animal combination and exercise study
High-exposure GW0742 liver and muscle toxicology
Primary preclinical study
Faiola B, Falls JG, Peterson RA, Bordelon NR, Brodie TA, Cummings CA, Romach EH, Miller RT. PPAR alpha, more than PPAR delta, mediates the hepatic and skeletal muscle alterations induced by the PPAR agonist GW0742. Toxicological sciences : an official journal of the Society of Toxicology. 2008. DOI 10.1093/toxsci/kfn130.
Ten-day controlled wild-type/PPAR-alpha-null mouse experiments found marked liver and muscle abnormalities at the highest exposure, with attenuated injury in knockout mice. This is compound-specific hazard evidence. The experimental exposures do not establish a human event rate, safe threshold or equivalence to chronic GW501516 carcinogenicity.
- Participants / model
- Male wild-type and PPAR-alpha-null mice; ten per genotype and treatment condition
- Treatment
- GW0742 and a PPAR-alpha comparator at toxicological exposures
- Follow-up
- 10 days
- Study design
- Controlled knockout-mechanism toxicology study
- Funding
- Industry-associated toxicology program
Nandhikonda et al. · high-concentration off-targets
Cell and biochemical receptor study
Nandhikonda P, Yasgar A, Baranowski AM, Sidhu PS, McCallum MM, Pawlak AJ, Teske K, Feleke B, Yuan NY, Kevin C, Bikle DD, Ayers SD, Webb P, Rai G, Simeonov A, Jadhav A, Maloney D, Arnold LA. Biochemistry. 2013. DOI 10.1021/bi400321p.
GW0742 weakly interacted with multiple nuclear receptors and became a broad nuclear-receptor antagonist above 12.1 micromolar in the reported cell and biochemical assays, with notable activity at vitamin D and androgen receptor systems.
- Participants / model
- Biochemical and cell receptor assays
- Treatment
- GW0742 across assay concentrations
- Study design
- High-throughput follow-up and receptor profiling
These receptor assays used cell concentrations; they do not establish an in vivo human interaction threshold.
Read the original sourceRussian GW0742/Fitorine rat epilepsy program, 2024
Primary preclinical study
Zubareva OE, Kharisova AR, Roginskaya AI, Kovalenko AA, Zakharova MV, Schwarz AP, Sinyak DS, Zaitsev AV. PPARβ/δ Agonist GW0742 Modulates Microglial and Astroglial Gene Expression in a Rat Model of Temporal Lobe Epilepsy. International journal of molecular sciences. 2024. DOI 10.3390/ijms251810015.
Seven-day treatment after lithium-pilocarpine injury partly altered behavior and astroglial/microglial expression. Behavioral groups were roughly 8 to 12 rats, with smaller endpoint-specific samples. The associated Russian proceedings describe the same research program and are not independent clinical replication.
- Participants / model
- Male Wistar rats, control and lithium-pilocarpine temporal-lobe-epilepsy groups
- Treatment
- GW0742/Fitorine 5 mg/kg/day for seven days versus vehicle
- Follow-up
- 7 days with subsequent behavior and tissue endpoints
- Study design
- Controlled four-group animal study
- Funding
- Russian Science Foundation project 23-25-00480
Kharisova et al. · Russian conference abstract
Preclinical rat study, Russian-language conference proceedings abstract
Харисова А.Р., Рогинская А.И., Захарова М.В., Шварц А.П., Зубарева О.Е. Биохимия человека: материалы всероссийской конференции с международным участием. 2024:78-79.
The Russian abstract describes male Wistar rats aged seven to eight weeks in a lithium-pilocarpine temporal-lobe-epilepsy model. Early GW0742 treatment altered selected glial activation and inflammatory-gene markers in hippocampus and temporal cortex.
- Participants / model
- Male Wistar rats aged 7 to 8 weeks
- Treatment
- Course of GW0742 during the first week after model induction
- Follow-up
- First week; latent-phase evaluation
- Study design
- Conference-abstract report of controlled animal work
- Funding
- Russian Science Foundation project 23-25-00480
The Russian-language proceedings overlap the later full paper and are not independent replication. The abstract does not report group size or GW0742 exposure.
Read the original sourceClinicalTrials.gov · no GW0742 study listed
Clinical trial registry
ClinicalTrials.gov records for GW0742, GW-0742, GW610742, and Fitorine.
ClinicalTrials.gov lists no study under GW0742, GW-0742, GW610742, or Fitorine. The cited public evidence also includes no human administration or concentration-time paper.
- Participants / model
- ClinicalTrials.gov records
- Treatment
- GW0742
Human evidence · no clinical performance result
PubMed and ClinicalTrials.gov records
PubMed and ClinicalTrials.gov records for GW0742 human administration and performance.
The cited records include no human administration, exercise, endurance, body-composition, or pharmacokinetic study. Human-cell studies do not constitute human clinical evidence.
- Participants / model
- Published and registered GW0742 records
WADA 2026 · PPAR-delta-agonist class applies
Official anti-doping standard
World Anti-Doping Agency. The 2026 Prohibited List, effective 1 January 2026.
Section S4.4.1 prohibits PPAR-delta agonists at all times using an including-but-not-limited-to list. It names GW1516/GW501516 as an example but does not name GW0742.
- Participants / model
- Athletes subject to the World Anti-Doping Code
- Follow-up
- Calendar year 2026
- Study design
- Anti-doping prohibited list
- Funding
- World Anti-Doping Agency
GW0742 class placement follows its primary PPAR-delta pharmacology; the named Cardarine example is a different molecule.
Read the original sourceChinese and Russian records · rat programs
Preclinical literature
Chinese and Russian literature and registry records for GW0742.
The cited Chinese record describes a China-affiliated acetaminophen acute-liver-injury mouse study. The cited Russian records describe the Saint Petersburg rat epilepsy program, including Russian proceedings and a peer-reviewed English paper. These sources include no human administration or pharmacokinetic result.
- Participants / model
- Chinese- and Russian-language literature and registry records
The Russian conference and index records overlap the peer-reviewed English paper and are not independent evidence. The Chinese registry record does not provide enough study detail to evaluate.
Read the original sourceChinese acetaminophen liver-injury study, 2024
Primary preclinical study
Wang L, Chen JH, Zhang YJ, Zhang MB, Zeng T. PPARβ/δ agonist GW0742 mitigates acute liver damage induced by acetaminophen overdose in mice. Toxicology and applied pharmacology. 2025. DOI 10.1016/j.taap.2024.117180.
Preventive and delayed GW0742 treatment improved selected biochemical and histological injury measures in mice, including treatment six hours after acetaminophen. This supports a disease-model hypothesis. It cannot be used to claim GW0742 is nonhepatotoxic in healthy users.
- Participants / model
- Male mice in an acetaminophen acute-liver-injury model
- Treatment
- Intraperitoneal GW0742 before or after acetaminophen, with vehicle and N-acetylcysteine comparisons
- Follow-up
- Acute injury experiment
- Study design
- Controlled preclinical disease-model study
PPAR-beta activation and AMPK subunits in muscle
Primary preclinical study
Lendoye E, Sibille B, Rousseau AS, Murdaca J, Grimaldi PA, Lopez P. PPARbeta activation induces rapid changes of both AMPK subunit expression and AMPK activation in mouse skeletal muscle. Molecular endocrinology (Baltimore, Md.). 2011. DOI 10.1210/me.2010-0504.
GW0742 rapidly changed AMPK subunit expression in mouse muscle and cultured myotubes. This provides a mechanistic link to oxidative remodeling, not a measured human performance outcome. A protein-expression response cannot be graded as endurance efficacy.
Read the original sourcePPAR-delta agonism, training and T-cell metabolism, 2021
Primary preclinical study
Sibille B, Mothe-Satney I, Le Menn G, Lepouse D, Le Garf S, Baudoin E, Murdaca J, Moratal C, Lamghari N, Chinetti G, Neels JG, Rousseau AS. Gene Doping with Peroxisome-Proliferator-Activated Receptor Beta/Delta Agonists Alters Immunity but Exercise Training Mitigates the Detection of Effects in Blood Samples. International journal of molecular sciences. 2021. DOI 10.3390/ijms222111497.
Human T cells were exposed in vitro; mice received six weeks of dietary GW0742 during an eight-week exercise program, with six animals per treatment group for the chronic experiment. Fatty-acid-oxidation potential increased, and combined treatment/training altered lymph-node Treg proportions. Blood signatures were partly masked by training. This expands mechanism and raises immunological questions; it did not demonstrate clinically important infection or immune harm in humans. The paper’s internet-dose discussion is not validated human PK.
Read the original sourceWhy is GW-0742 in D tier?
D: cell and animal effects, without human benefit or pharmacokinetic data in the cited evidence. GW-0742 alone was neutral on running time in the cited trained-mouse study; the large gain came from its AICAR combination. High-exposure mouse liver and muscle injury also matters.