GW-0742

GW-0742 is a lab-made molecule that switches on a cell receptor called PPARδ, and it’s a close chemical cousin of cardarine (GW-501516). It often gets sold and talked about next to SARMs and peptides in the “research chemical” world, but it’s neither of those — it’s a small-molecule that latches onto a receptor inside the cell. People get interested in it as an “exercise mimetic” (a drug meant to copy some effects of working out) because switching on PPARδ in muscle ramps up fat-burning. The catch: there are no human studies showing it works for anything, and the alarming cancer signal that killed its near-twin’s development is a serious, unanswered worry here too.

What it is

GW-0742 (also written GW0742; also known as GW610742, GW-0742X, GW610742X; CAS 317318-84-6) is a synthetic small molecule that turns on PPARδ (peroxisome proliferator-activated receptor delta, also called PPARβ/δ — a kind of molecular switch inside cells). It is not a peptide and not a SARM. SARMs act on the androgen receptor, and that isn’t what GW-0742 targets. It came out of the same GlaxoSmithKline/Ligand research program as GW-501516 (cardarine/endurobol) and was described in the same 2003 paper (GW-0742 = compound 7l; GW-501516 = 7k).

It’s one of the most precise PPARδ lab tools out there. It activates human PPARδ at roughly 1 nM EC50 (EC50 is the dose needed to get a half-strength effect — a lower number means more potent), and it’s about 1000 times more selective for PPARδ than for its cousins PPARα (EC50 ~1.1 µM) and PPARγ (EC50 ~2 µM). That makes it about as potent and selective as GW-501516. PPARδ is a switch that turns genes on or off, and it’s especially common in skeletal muscle, the heart, and other tissue that burns a lot of fuel. Flipping it on activates genes that burn fatty acids and boost the cell’s energy-producing machinery (PDK4, CD36, and the PGC-1α pathway), nudging the body toward burning fat for fuel. That’s the science behind the “exercise in a pill” pitch.

It isn’t perfectly tidy, though. At higher concentrations (above roughly 12 µM) GW-0742 starts to block several other cell receptors a little, hitting the vitamin D receptor (VDR) and androgen receptor (AR) hardest in cell-dish experiments (Nandhikonda et al., 2013). That’s worth keeping in mind when trying to make sense of any effect that isn’t coming from PPARδ.

The claims

In marketing and forum chatter, GW-0742 gets pitched as an “exercise mimetic” that delivers endurance, more stamina, fat loss, a shift toward more fat-burning muscle, and helpful metabolic effects — usually sold as “non-hormonal,” and often combined with or used in place of cardarine. All of these claims are stretched from rodent and cell experiments and from how PPARδ works in theory. None of them come from a human result.

What the evidence actually shows

Human evidence that it works is basically nonexistent. There are no human efficacy trials of GW-0742 for endurance, fat loss, recovery, longevity, looks, or anything else. The exercise-mimetic, muscle-fiber-shift, and fat-burning claims all rest on animal and cell studies:

• Endurance (mice): Turning on PPARδ with GW-0742 plus turning on AMPK (an energy-sensing switch) with AICAR boosted endurance in trained mice, along with gene-activity changes in muscle and liver (Manio et al., 2016).
• Cholesterol handling (mice): GW-0742 helped move cholesterol back out of the body in mice (Briand et al., 2009).
• Heart and lungs (rats): Oral GW-0742 for three weeks reduced thickening of the heart’s right side and lowered pressure there in a rat model of high blood pressure in the lungs caused by low oxygen (PLOS One, 2010).
• Off-target (cell-based): Weakly blocked several other cell receptors, hitting VDR and AR hardest (Nandhikonda et al., 2013).

The only human data that exists is about detection, not treatment. In an anti-doping study, subjects were given a single oral dose of GW-0742 (and GW-1516) so labs could map out what the body excretes in urine. That study shows the drug can be detected — its sulfone breakdown products are trackable for about 20 days for GW-0742, at levels roughly 10× lower than for GW-1516 — but it says nothing about whether the drug is effective or safe as a performance or longevity aid (Sobolevsky et al., 2012).

Legal and regulatory status

GW-0742 is a research-grade chemical only. It’s not an approved drug anywhere, it has no ATC code (an official drug classification number), and it’s not a legitimate supplement, cosmetic, or food ingredient. Lab-supply companies sell it strictly as a research tool labeled “for research use only — not for human use.” It was studied in early lab and animal research, but there’s no sign it ever moved into a real human treatment program, and no clinical-trial (NCT) records were found for it.

Anti-doping (WADA): GW-0742 is prohibited at all times — both in and out of competition — under Section S4 (Hormone and Metabolic Modulators), in the Metabolic Modulators subsection, which bans PPARδ agonists as a whole class (with GW-1516/cardarine as the named example). On the current (2026) list this sits at S4.4.1, grouped with AMPK activators such as AICAR. WADA has renumbered this subsection over the years (it’s also been listed as S4.4 and S4.5 in different years), but PPARδ agonists as a class have always been covered, so GW-0742 falls under the same ban. This is the same class entry that bans cardarine, and it’s separate from SARMs, which sit under S1.2 (Anabolic Agents). Urine tests that can spot GW-0742 already exist.

Safety

There is no human safety data for GW-0742 beyond the small doping-detection excretion study, so its long-term safety in people is simply unknown.

The big red flag comes by comparison. Its near-twin GW-501516 had its drug development dropped by GSK around 2006–2007 after long-term (roughly two-year) rodent studies showed cancers developing quickly across multiple organs — a finding backed up by USADA and Sport Integrity Australia. That clearly documented multi-organ cancer study is for GW-501516; there doesn’t seem to be an equally solid, standalone long-term cancer study published specifically for GW-0742. But GW-0742 is a structurally and mechanistically equivalent potent PPARδ agonist, so you can’t assume the cancer signal doesn’t apply here. Treat the cancer risk as a serious, unresolved concern.

Lab and cell data also flag built-in toxicity with longer exposure — for example, it protected nerve cells at a brief (12 h) exposure but became toxic by 48 h in cerebellar granule neuron cultures (a type of brain-cell culture), according to supplier testing. And the off-target blocking of VDR and AR adds more uncertainty about what it does beyond its intended target.

Bottom line

GW-0742 is a non-peptide, non-SARM PPARδ agonist and a close cousin of cardarine, with interesting rodent and cell data but no human evidence that it works and no human safety data. It’s an unapproved research chemical with no legitimate role in people, and it’s banned in sport at all times. Most importantly, its near-twin’s development was abandoned over multi-organ cancer in long-term animal studies — a warning sign that can’t be assumed to skip a chemically and biologically equivalent compound. Evidence for any biohacking, longevity, or performance benefit in humans is thin to nonexistent.

Evidence grade: 3/10 · Animal only.

Sources

• Sznaidman ML et al. (2003), Bioorg Med Chem Lett — PMID 12699745
• Sobolevsky T et al. (2012), Drug Test Anal — PMID 22977012
• Manio MCC et al. (2016), Physiol Rep — PMC4823600
• Briand F et al. (2009), Clin Transl Sci — PMID 20169010
• Nandhikonda P et al. (2013), Biochemistry — PMC3724348
• Harrington LS et al. (2010), PLOS One — PMC2831997
• WADA Prohibited List (S4 Hormone and Metabolic Modulators)
• USADA — What Should Athletes Know About GW1516?
• Sport Integrity Australia — GW1516 information