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GW-0742

Also known as gw 610742, fitorine · Wikipedia

GW-0742 (sometimes labelled GW-610742) is a small-molecule selective PPAR-delta (PPARbeta/delta) agonist developed as a research tool compound - it is NOT a peptide. Preclinical studies have characterised it as an exercise-mimetic that upregulates fatty-acid oxidation, mitochondrial biogenesis, and oxidative muscle-fiber gene programs, and exerts anti-inflammatory effects via NF-kB suppression (Cheng et al., 2004; Sahebkar et al., 2014). Its structural sister molecule, GW-501516 (cardarine), caused multiple tumour types in long-term rodent carcinogenicity studies, and GSK halted that program. GW-0742 has no human clinical trial development and is sold only as a research chemical. WADA prohibits PPAR-delta agonists at all times (S4.5).

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Mechanism of action

GW-0742 is a small-molecule selective agonist of the peroxisome proliferator-activated receptor delta (PPAR-delta / PPAR-beta), with high selectivity over PPAR-alpha and PPAR-gamma. Activated PPAR-delta heterodimerises with RXR and binds peroxisome proliferator response elements (PPREs) on target genes.

GW-0742 is a small-molecule selective agonist of the peroxisome proliferator-activated receptor delta (PPAR-delta / PPAR-beta), with high selectivity over PPAR-alpha and PPAR-gamma. Activated PPAR-delta heterodimerises with RXR and binds peroxisome proliferator response elements (PPREs) on target genes. In skeletal muscle, liver, cardiomyocytes, and adipose tissue, this upregulates fatty-acid uptake and beta-oxidation enzymes (CPT-1, ACOX1), mitochondrial biogenesis via PGC-1alpha, and a shift toward type I oxidative fibres (Cheng et al., Circulation Research 2004; Burkart et al.). PPAR-delta activation also suppresses NF-kB-mediated inflammatory transcription and has shown cardioprotection in rodent ischaemia/reperfusion models. The mechanism overlaps closely with the sister compound GW-501516 (cardarine), differing mainly in receptor binding kinetics and off-target profile.

Pharmacokinetic properties

Half-life

Approximately 8-24 hours in preclinical models; human PK not characterized

Routes

oral

Bioavailability

Designed as an orally bioavailable small molecule; standard formulations are oral tablets/suspension. No injectable use rationale.

Amino-acid sequence

[4-[[[2-[3-Fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl]methyl]thio]-2-methylphenyloxy]acetic acid

Use & research dosing

There is no human clinical dose for GW-0742. Preclinical rodent studies have generally used 1-10 mg/kg/day orally for short courses. Self-experimentation protocols, where they exist, are typically modelled on cardarine (GW-501516) at 5-15 mg/day orally for cycles of 4-8 weeks. These protocols are not supported by any controlled human PK, safety, or efficacy data, and the rodent carcinogenicity signal seen with the sister molecule GW-501516 should be assumed to apply to this class until proven otherwise. No formal dose-finding has been performed.

Research-use framing only. SavePeptides sells nothing for human consumption. Doses above reflect reported research / self-experimentation ranges, not clinical recommendations.

Editorial perspective

Knowledge-base content for GW-0742 must clearly flag two things: (1) it is not a peptide - it is a small-molecule PPAR-delta agonist - and (2) the structurally related cardarine (GW-501516) caused multiple tumour types in long-term rodent carcinogenicity studies, leading GSK to halt development; WADA has issued an explicit health-risk alert about cardarine. GW-0742 cannot be assumed safe by analogy. There is no IND-stage clinical program. All sales are research-only.

— SavePeptides editorial desk · last updated 2026-05-25

Cautions & contraindications

Before researching this compound, note:

  • NOT a peptide - small-molecule PPAR-delta agonist (knowledge-base flag)
  • Prohibited by WADA at all times (S4.5 metabolic modulators) - disqualifying for tested athletes
  • Significant theoretical and class-level cancer risk: the structurally related GW-501516 (cardarine) caused multiple tumour types in 2-year rodent carcinogenicity studies, leading GSK to halt development
  • No completed human clinical trials; no validated human safety data
  • Unknown drug interactions; PPAR-delta is widely expressed (muscle, liver, heart, vasculature, skin, immune cells)
  • Avoid in pregnancy, lactation, and any personal or family history of malignancy
  • Hepatic and cardiovascular safety not characterised in humans
  • Vendor product is research-grade with no quality oversight; identity and purity not assured

Facts verified

2026-05-25

Confidence

low

What this means

  • NOT a peptide - small-molecule PPAR-delta agonist
  • sister molecule cardarine (GW-501516) caused tumours in 2-year rodent carcinogenicity studies; class-level cancer risk concern
  • no human clinical trials; no human safety data
  • WADA prohibited at all times (S4.5)

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GW-0742 · SavePeptides