What is the difference between GW-0742 and Meldonium?

GW-0742: GW-0742 is a synthetic small-molecule PPARδ (PPAR-beta/delta) agonist developed by GlaxoSmithKline as a phenoxyacetic-acid/thiazole derivative—not a peptide or hormone. It exhibits ~1000-fold selectiv... Meldonium: Meldonium (Mildronate) is a small-molecule carnitine-biosynthesis inhibitor and anti-ischemic metabolic modulator — not a peptide. It is an approved prescription drug for cardiovascular indications in...

What does the research say about GW-0742 vs Meldonium?

GW-0742: No human efficacy or safety data exist; the only identified human exposure is a single 15 mg oral dose administered to volunteers solely to characterize urinary metabolites for an anti-doping detection assay—a bioanalytical study yielding no therapeutic or safety information. Preclinical rodent findings include: oral GW-0742 (30 mg/kg/day × 3 weeks… Meldonium: In rat ischemia-reperfusion models, meldonium (100–200 mg/kg) reduced myocardial infarct size ~30% and protected liver, brain, and endothelial function. In humans it is used clinically (in approving markets) for chronic heart failure and angina at 500 mg twice daily, but there is no FDA/EMA-registered pivotal efficacy trial. Urinary detection persi…

GW-0742 vs Meldonium

Q: Can you stack GW-0742 and Meldonium?

GW-0742 (metabolic) and Meldonium (metabolic) are in the same category and may have overlapping mechanisms — researchers should review both profiles carefully before combining. Consult a licensed provider before combining any compounds.

Head-to-head comparison of GW-0742 and Meldonium — mechanism, side effects, legal status, and pricing.

GW-0742

GW-0742 is a synthetic small-molecule PPARδ (PPAR-beta/delta) agonist developed by GlaxoSmithKline as a phenoxyacetic-acid/thiazole derivative—not a peptide or hormone. It exhibits ~1000-fold selectivity for human PPARδ (EC50 = 1.1 nM) over PPARα and PPARγ. Never advanced past preclinical development, GW-0742 has no approved human therapeutic use and no registered clinical trials. It is prohibited at all times under WADA as a member of the banned PPARδ-agonist class (Hormone and Metabolic Modulators), though not individually named on the list.

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Meldonium

Meldonium (Mildronate) is a small-molecule carnitine-biosynthesis inhibitor and anti-ischemic metabolic modulator — not a peptide. It is an approved prescription drug for cardiovascular indications in several ex-Soviet states but is not FDA- or EMA-approved, and it is WADA-prohibited (added January 2016, of Sharapova notoriety). It is also sold as a gray-market research chemical.

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GW-0742

Meldonium

Category

Metabolic

Legal Status

Research Only

Mechanism

GW-0742 is a high-affinity, highly selective agonist of human PPARδ (EC50 = 1.1 nM for hPPARδ transactivation vs ~1.1 µM for hPPARα and ~2 µM for hPPARγ), conferring ~1000-fold selectivity for PPARδ over the other PPAR subtypes. Upon activation, PPARδ heterodimerizes with RXR and binds PPAR-response elements (PPREs) to alter transcription of genes governing fatty-acid oxidation, glucose utilization, and inflammatory signaling. In mice, however, GW-0742-induced hepatomegaly, hepatic/skeletal-muscle peroxisome proliferation, and skeletal myopathy were shown to be predominantly mediated by off-target PPARα cross-activation rather than PPARδ—a mechanism-based toxicity concern at animal-study exposures.

Meldonium competitively inhibits γ-butyrobetaine hydroxylase — the enzyme that makes L-carnitine — and the carnitine transporter OCTN2, lowering intracellular L-carnitine. Reduced carnitine suppresses long-chain fatty-acid β-oxidation and shifts energy metabolism toward glycolysis, an effect proposed to be anti-ischemic/cardioprotective (Dambrova et al., 2016).

Side Effects

Hepatomegaly (liver enlargement) observed in mice
Hepatic and skeletal-muscle peroxisome proliferation (mouse studies)
Skeletal myopathy driven by off-target PPARα cross-activation (mouse studies)
No human safety data beyond single-dose bioanalytical exposure

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GW-0742

Best $/mg

$0.058/mg

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Meldonium

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Lab Verification

COA corpus from Disclosed Labs — independently tested batches only.

GW-0742

COAs

99.6%

Avg purity

Labs

Full testing data

Meldonium

COAs

99.9%

Avg purity

Labs

Full testing data

GW-0742 Research Summary

No human efficacy or safety data exist; the only identified human exposure is a single 15 mg oral dose administered to volunteers solely to characterize urinary metabolites for an anti-doping detection assay—a bioanalytical study yielding no therapeutic or safety information. Preclinical rodent findings include: oral GW-0742 (30 mg/kg/day × 3 weeks) reduced right ventricular hypertrophy and systolic pressure in rats with chronic hypoxia-induced pulmonary hypertension but did not prevent pulmonary vascular remodeling; intraperitoneal GW-0742 (0.1 mg/kg) improved survival and reduced intestinal injury, leukocyte activation, cytokines, and apoptosis markers in a mouse gut ischemia/reperfusion model; and GW-0742 ameliorated hepatic steatosis, ER stress, and lung inflammation in various mouse models. Critically, mouse studies also demonstrated hepatomegaly, hepatic/skeletal-muscle peroxisome proliferation, and skeletal myopathy driven predominantly by off-target PPARα cross-activation, indicating mechanism-based toxicity risk.

Key references

Meldonium Research Summary

In rat ischemia-reperfusion models, meldonium (100–200 mg/kg) reduced myocardial infarct size ~30% and protected liver, brain, and endothelial function. In humans it is used clinically (in approving markets) for chronic heart failure and angina at 500 mg twice daily, but there is no FDA/EMA-registered pivotal efficacy trial. Urinary detection persists for weeks-to-months, central to doping cases. Not FDA/EMA-approved; not a peptide.

Key references

Can you stack GW-0742 and Meldonium?

GW-0742 and Meldonium are both in the Metabolic category and may have overlapping mechanisms. Researchers should review both profiles carefully, understand the mechanisms of action, and monitor the relevant biomarkers when combining compounds in the same class. As always, consult a licensed healthcare provider before making any decisions about combining research compounds.

Other comparisons

Meldonium vs MOTS-c GW-0742 vs MOTS-c AOD-9604 vs Meldonium AOD-9604 vs GW-0742 5-Amino-1MQ vs Meldonium 5-Amino-1MQ vs GW-0742 Meldonium vs NAD+GW-0742 vs NAD+

This platform provides informational tools only, not medical advice. This comparison is for educational purposes only. Consult a licensed provider.