GW-0742

Overview

GW-0742 (also GW0742, GW610742, GW610742X) is a synthetic nonsteroidal small-molecule agonist of the peroxisome proliferator-activated receptor delta (PPARδ, also called PPARβ/δ) — a nuclear hormone receptor that regulates lipid-metabolism genes. It was first described by GlaxoSmithKline (Sznaidman et al., 2003) as a highly selective research-tool compound for probing PPARδ biology.

Two things it is not:

• NOT a peptide. It is a lab-made small molecule (C21H17F4NO3S2), not an amino-acid chain. It appears in this peptide reference only because it is discussed and stacked alongside peptides in the fitness and "research chemical" community.
• NOT a SARM. SARMs (selective androgen receptor modulators) act on the androgen receptor; GW-0742 acts on PPARδ, an entirely different nuclear receptor. Despite being marketed online as an "endurance/fat-loss SARM," that label is mechanistically wrong.

GW-0742 is essentially a close structural analog of cardarine (GW-501516), from which it differs by a single extra fluorine atom. Because of that near-identity, most of the "benefits" attributed to GW-0742 are actually borrowed from cardarine's and the wider PPARδ class's animal data — and so is the class's central safety problem.

Chemistry and structure

GW-0742 is a small-molecule thiazole/fluorinated compound, not an amino-acid chain.

Mechanism of action

• High-affinity, highly selective PPARδ (PPARβ/δ) agonist. GW-0742 binds and activates PPARδ, a nuclear hormone receptor that binds DNA and drives transcription of lipid-metabolism genes. Reported transactivation EC50 is roughly ~1 nM for human PPARδ versus ~1–2 µM for PPARα and PPARγ (on the order of ~300–1,000-fold selectivity). [In vitro]
• Fatty-acid oxidation / oxidative-muscle program. It upregulates fatty-acid-oxidation genes (e.g. CPT1a, a rate-limiting enzyme of fatty-acid oxidation) and shifts skeletal muscle toward an oxidative/endurance program — the same transcriptional axis studied with cardarine. [Animal]
• Anti-inflammatory signaling. In rodent models of colitis and neuroinflammation it reduced inflammatory markers (TNF-α, IL-6, IL-1β). [Animal]
• Cardiac fatty-acid oxidation / ischemia protection. In cardiomyocytes it increased fatty-acid oxidation and protected against ischemia–reperfusion injury. [Animal]
• Not an androgen-receptor mechanism. GW-0742 is not a SARM and not a peptide — it is mechanistically distinct from androgen-based muscle-building compounds, despite being marketed as an "endurance/fat-loss SARM." [In vitro]

Research and evidence

Human evidence in context. GW-0742 has never been tested in a human clinical trial — there is no registered Phase 1 study and no human pharmacokinetic, efficacy, or safety data. The endurance/metabolic claims circulating online largely derive from the cardarine (GW-501516) and broader PPARδ-class literature, not from robust GW-0742-specific human data. In fact, GW-0742 has a thinner data set than cardarine, which at least reached Phase 1/2 before being abandoned. Human bioavailability, half-life, effective dose, and adverse-effect profile were not found in these sources.

Status and regulation

• Regulatory approval: None. GW-0742 is not approved by the FDA, EMA, or any other regulator for any indication, and it was never developed as a drug — it has always been a research-tool compound. Its highest development phase is none (preclinical only).
• Anti-doping: GW-0742 falls under the World Anti-Doping Agency (WADA) Prohibited List, Class S4.4 (Metabolic Modulators — PPARδ agonists) and is prohibited at all times in sport. WADA is a separate axis from legality — sport-eligibility, not a legal classification.
• Market reality: It is sold only as a research reagent and circulates online, frequently mislabeled as a "SARM." Such products are of unknown identity, purity, and potency.

Safety

Contamination reality. Products sold as "SARMs" frequently do not contain the labeled compound. Van Wagoner et al. (JAMA 2017;318(20):2004-2010; PMID 29183075) tested 44 products sold as SARMs: only 52% contained the labeled SARM, 39% contained a different unapproved drug, and 9% contained no active drug at all. A "GW-0742" label is therefore not a reliable statement of contents — mislabeling, contamination, and incorrect dosing are additional, separate hazards on top of the compound's own unknowns.

Legal status

How it compares

• Cardarine — GW-0742's near-twin: the same PPARδ agonist class, differing by one fluorine atom. Cardarine at least reached short human Phase 1/2 lipid trials before GSK abandoned it over rodent multi-organ tumors; GW-0742 has an even thinner, preclinical-only data set but shares the same mechanism and cancer concern.
• Stenabolic (SR9011) — another non-SARM "endurance/metabolic" research compound often grouped with GW-0742. It acts on Rev-ErbA, not PPARδ or the androgen receptor, and is likewise preclinical-only and not a peptide.

See the Weight management overview for how these metabolic research compounds are framed.

Common misconceptions

• "GW-0742 is a SARM." No. SARMs act on the androgen receptor; GW-0742 is a PPARδ agonist. It is sold alongside SARMs, which is the source of the confusion, but the mechanism is entirely different.
• "GW-0742 is a peptide." No. It is a synthetic small molecule (C21H17F4NO3S2, 471.5 g/mol). It is covered here only because it is discussed and stacked with peptides.
• "It's basically a safer, newer cardarine." Not established. It differs from cardarine by one fluorine atom and shares the same PPARδ mechanism and class-based cancer concern — with an even thinner (preclinical-only, no-human) data set. Nothing shows it is safer.
• "Human research proved it boosts endurance and fat loss." No. There is no human GW-0742 data at all. Those claims are borrowed from cardarine and the PPARδ class, largely from animal studies.

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This entry is educational and summarizes published research and public regulatory information. It is not medical advice, a recommendation, or a guide to obtaining or using any substance. Not legal advice — check the rules of your own jurisdiction.