In mice, the PPARδ agonist GW501516 increased running endurance and reproduced several effects of endurance training, coining the term 'exercise mimetic.'
Cardarine (GW501516)

WADA BANNED - Prohibited in competitive sports as metabolic modulator
Overview
Last reviewed: 2026-08-18
Identity & Aliases
Also known as
Status: Research compound - PPAR-delta agonist
Full composition (formula, molecular weight, sequence) in Quick Facts →
Research Areas
Available Evidence
One short-term randomized controlled trial in moderately obese men found that the PPARδ agonist GW501516 improved several metabolic parameters (reduced plasma triglycerides, improved markers of insulin resistance, increased fat oxidation) — but it was a small, short-duration study, not a clinical development program.
A landmark mouse study showed GW501516 increased running endurance substantially and, together with AMPK activators, was described as an 'exercise mimetic.' Long-term rodent toxicology reportedly showed increased tumor incidence in multiple organs, leading the developer to halt clinical development.
Cell-based assays characterize GW501516 as a potent, selective PPARδ agonist that drives expression of genes involved in fatty acid oxidation.
The tumor findings that ended development were widely reported but were not published as a full peer-reviewed toxicology paper; long-term human safety and efficacy are therefore unknown, and online 'cardarine' use rests on animal data plus community anecdote.
Key Studies & Findings
In a short-term randomized controlled trial in moderately obese men, PPARδ activation with GW501516 reversed multiple metabolic abnormalities, reduced oxidative stress, and increased fatty acid oxidation.
Benefits & Effects
Side Effects & Safety
SEVERE/FATAL side effect
Onset: 104 weeks (animal)
Management: DO NOT USE - No approved treatment
Dose-dependent
Severe side effect
Onset: During pregnancy
Management: CONTRAINDICATED
Dose-dependent
Limitations & Open Questions
Pharmacology
Reported Research Dosing
Reported values from research literature and community protocols. Educational reference only — not a dosing recommendation or medical advice.
10-20mg daily
Frequently Asked Questions
Is cardarine a SARM?
No. Cardarine (GW501516) is a PPARδ receptor agonist, not an androgen-receptor modulator; it is often mislabeled in fitness communities.
Why was GW501516 development stopped?
Long-term rodent studies reportedly found tumors in multiple organs; the developer discontinued clinical development and the compound was never approved for any indication.
Is cardarine safe for humans?
That is unknown. Human data are limited to a short-term trial, and animal carcinogenicity signals mean long-term risk cannot be ruled out; it remains a research compound.
Research Citations
Kintz P, Ameline A, Gheddar L, Raul JS (2020)
Chong S, Woolnough CA, Koyyalamudi SR, Perera NJ (2024)
Lefere S, Puengel T, Hundertmark J, Penners C, Frank AK, Guillot A, de Muynck K, Heymann F, Adarbes V, Defrêne E, Estivalet C, Geerts A, Devisscher L, Wettstein G, Tacke F (2020)
Turza A, Pascuta P, Muresan-Pop M, Mare L, Borodi G, Popescu V (2024)
+ 33 more citations
Related Resources
Quick Facts
Formula
C21H18F3NO3S2
Molecular Weight
453.50
Mechanism
PPAR-delta agonist for endurance enhancement
Safety Information
Research compound only. Animal studies raised concerns about tumor development at high doses.
Citations
38Kintz P, Ameline A, Gheddar L, Raul JS (2020)
Chong S, Woolnough CA, Koyyalamudi SR, Perera NJ (2024)
Lefere S, Puengel T, Hundertmark J, Penners C, Frank AK, Guillot A, de Muynck K, Heymann F, Adarbes V, Defrêne E, Estivalet C, Geerts A, Devisscher L, Wettstein G, Tacke F (2020)
Turza A, Pascuta P, Muresan-Pop M, Mare L, Borodi G, Popescu V (2024)
+ 33 more citations