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GW0742 1g

GW0742 1g

€55,00 EUR
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                                          NOT FOR HUMAN CONSUMPTION

GW0742 is a highly selective agonist of PPARβ/δ (a nuclear receptor abundant in skeletal muscle, endothelium, liver, and macrophages). Activation upshifts fatty-acid oxidation (FAO) and mitochondrial programs (PGC-1α), improves insulin sensitivity, and exerts anti-inflammatory/vasculoprotective effects via transrepression of NF-κB/AP-1. It is not approved for human use (preclinical tool compound) and PPARδ modulators are prohibited by WADA.

Additional Benefits of GW0742 Now Under Investigation

Benefit Key take-aways
1 Endurance & muscle metabolic reprogramming Up-regulates CPT-1, PDK4, UCP3, shifts fibers toward oxidative/type I phenotype; improves time-to-exhaustion in rodents—an “exercise-mimetic” signature.
2 Insulin sensitivity Enhances glucose tolerance/HOMA-IR, increases muscle FAO, and reduces lipotoxic intermediates in diet-induced obesity models.
3 Atheroprotection & lipids Promotes cholesterol efflux (ABCA1/ABCG1), lowers TG/non-HDL, and reduces vascular inflammation; smaller plaques in hyperlipidemic mice.
4 Endothelial function Increases eNOS/NO bioavailability, lowers VCAM-1/ICAM-1, improving microvascular responses in models.
5 NAFLD/MASH signals Decreases hepatic steatosis via ↑ β-oxidation and ↓ DNL; lowers ALT/AST and inflammatory transcripts in preclinical liver disease.
6 Anti-inflammatory in gut/systemic Restraints NF-κB cytokines (TNF-α, IL-6); ameliorates colitis severity with better barrier proteins.
7 Renal protection Mitigates ischemia–reperfusion and diabetic-nephropathy injury via mitochondrial preservation and anti-fibrotic signaling.
8 Pulmonary hypertension/fibrosis Lowers RV pressure and vascular remodeling in PAH; attenuates TGF-β–drivenfibroblast activation.
9 Neuroprotection (preclinical) Improves neuronal mitochondrial function, reduces microglial cytokines, benefits motor/cognitive readouts in toxin/aging models.

2. Molecular Mechanism of Action

2.1 Receptor pharmacodynamics

  • PPARβ/δ–RXR heterodimer → PPRE transcription of FAO/mitochondrial genes (PGC-1α, CPT-1, ACO, UCP3).

  • Transrepression: Interferes with NF-κB/AP-1 → ↓ inflammatory gene expression (COX-2, TNF-α).

  • Macrophages: ↑ ABCA1/ABCG1 efflux; M2-like shift.

  • Endothelium: ↑ eNOS, ↓ adhesion molecules → vasoprotection.

2.2 Down-stream biology

Pathway Functional outcome Context
FAO/PGC-1α program ↑ Oxidative metabolism, endurance Skeletal muscle
ABCA1/ABCG1 ↑ Cholesterol efflux, ↓ foam cells Atherogenesis
NF-κB/AP-1 restraint ↓ Cytokines/adhesion Vascular & gut
eNOS activation ↑ NO, endothelial function CV system
Anti-fibrotic (TGF-β axis) ↓ Collagen deposition Kidney/lung/heart

3. Pharmacokinetics (preclinical)

  • Route: Oral in animal studies.

  • Exposure: Hours-scale half-life in rodents; species-dependent bioavailability.

  • Metabolism: Likely hepatic oxidation; human PK unknown.

4. Evidence Summary

  • Metabolic disease: Consistent insulin-sensitizing and anti-steatotic effects with improved muscle FAO/glucose uptake in rodents.

  • Cardiovascular: Reduced atherosclerotic plaque, improved endothelial function, anti-remodeling post-injury.

  • Renal/pulmonary/gut/CNS: Protection across models via mitochondrial and anti-inflammatory mechanisms.

Evidence quality note: Strong mechanistic + animal data; no peer-reviewed human efficacy trials with GW0742.

5. Emerging Clinical Interests (conceptual)

Field Rationale Status
Obesity/insulin resistance Muscle FAO & metabolic flexibility ↑ Preclinical
Atherosclerosis prevention Efflux + anti-inflammatory Preclinical
NAFLD/MASH Anti-steatotic + anti-inflammatory Preclinical
PAH/fibrosis Vascular & fibroblast modulation Preclinical
IBD Barrier + cytokine restraint Preclinical
Neurodegeneration Mitochondrial/anti-inflammatory Preclinical

6. Safety & Tolerability

  • Human safety: Unknown.

  • Class concern: Another PPARδ agonist (GW501516) produced rodent tumorigenesis at high exposures/long durations; though GW0742 differs, long-term oncogenic risk is unresolved for the class.

  • Metabolic drift: Likely HDL↑/TG↓ benefits; off-target hepatic/lipid effects at supraphysiologic doses possible.

  • Sport/anti-doping: PPARδ agonists are banned; detection programs exist.

  • Drug interactions: Potential nuclear-receptor/CYP/transporter cross-talk—uncharacterized clinically.

Comparative matrix

Feature GW0742 (PPARδ) GW501516 (PPARδ) Fenofibrate (PPARα)
Human approval No No Yes
Selectivity High for δ High for δ α
Endurance/FAO Strong (preclinical) Strong (preclinical) Mild (liver-centric)
Tumor signal (rodent) Unknown Present None δ-class

7. Regulatory Landscape

  • Status: Preclinical research tool; not a medicine or supplement.

  • WADA: Prohibited (metabolic modulators).

8. Practical Take & Future Directions

  • Today: Laboratory mechanistic studies only; not for human self-use.

  • Needed next: Drug-like δ-agonists with safety windows, GLP tox/carcinogenicity, and PoM/PoC trials using metabolic and vascular endpoints plus omics/biopsy markers.

  • Opportunities: Tissue-targeted or biased PPARδ modulators to capture FAO/mitochondrial gains while minimizing proliferative risk.

Selected References

  • Muscle oxidative switch & FAO gene programs (PPARδ/PGC-1α): Cell Metabolism; Nature Medicine.

  • PPARδ in insulin resistance & NAFLD: Hepatology; Gastroenterology.

  • Vascular/endothelial protection & atherogenesis: Circulation; ATVB; JCI.

  • Colitis/IBD and anti-inflammatory effects: Gut; PNAS.

  • Renal, pulmonary, and cardiac remodeling models: Kidney Int; Am J Respir Crit Care Med; Cardiovasc Res.

  • WADA/anti-doping overview: Drug Testing & Analysis; WADA Code.