What is the difference between AICAR and GW-0742?

AICAR: AICAR (acadesine / AICA riboside) is a purine nucleoside analog and AMP-mimetic — not a peptide — that activates AMPK. Studied in registered human trials under the name acadesine (for cardioprotection... 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...

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

AICAR: As acadesine, AICAR was tested in registered human trials by IV infusion: the large RED-CABG cardioprotection trial (JAMA 2012) was stopped for futility, and a Phase I/II study in relapsed/refractory CLL established 210 mg/kg IV as the optimal dose. No human trial evaluated AICAR for exercise, fat loss, or longevity, and no validated non-IV dosing… 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…

AICAR vs GW-0742

Q: Can you stack AICAR and GW-0742?

AICAR (metabolic) and GW-0742 (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 AICAR and GW-0742 — mechanism, side effects, legal status, and pricing.

AICAR

AICAR (acadesine / AICA riboside) is a purine nucleoside analog and AMP-mimetic — not a peptide — that activates AMPK. Studied in registered human trials under the name acadesine (for cardioprotection and leukemia, not performance), it is not FDA-approved for any indication and is WADA-prohibited at all times. It is sold on the gray market as an "exercise mimetic."

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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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AICAR

GW-0742

Category

Metabolic

Legal Status

Research Only

Mechanism

AICAR is taken into cells and phosphorylated to ZMP, an AMP-mimetic that allosterically activates AMPK (binding the γ-subunit CBS domains and protecting Thr172 from dephosphorylation). Because ZMP can reach millimolar levels, AICAR also has substantial AMPK-independent effects on other AMP-sensitive enzymes and nucleotide metabolism (Visnjic et al., 2021). In sedentary mice, 4 weeks of AICAR increased treadmill endurance ~44% (Narkar et al., Cell 2008).

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.

Side Effects

In supervised IV trials: hyperuricemia (managed with allopurinol), transient creatinine elevation, infusion-related hypotension, mild transient anemia/thrombocytopenia
The large RED-CABG cardioprotection trial was stopped for futility — no demonstrated benefit

Where Researchers Are Buying

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COA-verified vendors · trust score ≥70 required · single-vial price — bulk/bundle deals may be lower

AICAR

Best $/mg

$0.800/mg

Kimera ChemsC

2 trusted vendors listing

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GW-0742

Best $/mg

$0.058/mg

Kimera ChemsC

1 trusted vendor listing

Compare all 1 vendor

Lab Verification

COA corpus from Disclosed Labs — independently tested batches only.

AICAR

COAs

99.3%

Avg purity

Labs

Full testing data

GW-0742

COAs

99.6%

Avg purity

Labs

Full testing data

AICAR Research Summary

As acadesine, AICAR was tested in registered human trials by IV infusion: the large RED-CABG cardioprotection trial (JAMA 2012) was stopped for futility, and a Phase I/II study in relapsed/refractory CLL established 210 mg/kg IV as the optimal dose. No human trial evaluated AICAR for exercise, fat loss, or longevity, and no validated non-IV dosing exists. Not FDA-approved; not a peptide.

Key references

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

Novel selective small molecule agonists for peroxisome proliferator-activated receptor δ (PPARδ) — synthesis and biological activity (2003)

Can you stack AICAR and GW-0742?

AICAR and GW-0742 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

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