Name: GW0742 100x10mg
Brand: Averlane Labs
Price: 75.00 EUR
Availability: InStock

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.

GW0742 100x10mg

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