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Cardarine (GW501516)

Cardarine (GW501516) molecular structure

WADA BANNED - Prohibited in competitive sports as metabolic modulator

Overview

Cardarine (GW501516) is not a peptide but a synthetic peroxisome proliferator-activated receptor delta (PPARδ) agonist originally developed for metabolic and cardiovascular diseases. PPARδ activation increases fatty acid oxidation, improves lipid profiles, enhances endurance capacity, and promotes fat metabolism over glucose utilization. Research demonstrated dramatic increases in running endurance in animal studies without exercise training. The compound improves insulin sensitivity, raises HDL cholesterol, and lowers triglycerides. However, development was discontinued after long-term rodent studies showed increased cancer incidence in multiple organs. Despite these safety concerns, Cardarine remains popular in fitness communities for its perceived fat-burning and endurance-enhancing effects. The compound is banned by WADA for competitive athletes. Given the carcinogenicity signals in animal studies, Cardarine carries significant potential risks that have not been evaluated in long-term human trials. The compound is sometimes mistakenly grouped with SARMs despite having a completely different mechanism of action.

Last reviewed: 2026-08-18

Identity & Aliases

Also known as

GW501516GW-501516GSK-516Endurobol

Status: Research compound - PPAR-delta agonist

CAS317318-70-0
PubChem9803963

Full composition (formula, molecular weight, sequence) in Quick Facts →

Research Areas

Endurance and exercise mimeticsLipid metabolism / metabolic syndromePPARδ receptor pharmacologyFatty acid oxidation

Available Evidence

Human

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.

Animal

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.

In Vitro

Cell-based assays characterize GW501516 as a potent, selective PPARδ agonist that drives expression of genes involved in fatty acid oxidation.

Uncertain

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

2 studies
Preclinical2008

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

Clinical2008

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

6 documented

Enhanced endurance

anecdotal

Fat burning

anecdotal

Improved lipid profile

anecdotal

Increased HDL cholesterol

anecdotal

Metabolic optimization

anecdotal

Exercise performance

anecdotal

Side Effects & Safety

6 reported

Long-term safety concerns

MildUncommon

Potential tumor risk at high doses

MildUncommon

Headache

MildUncommon

SEVERE/FATAL side effect

SEVERE/FATALVery high in animals

Onset: 104 weeks (animal)

Management: DO NOT USE - No approved treatment

Dose-dependent

Severe side effect

SevereDocumented

Onset: During pregnancy

Management: CONTRAINDICATED

Dose-dependent

Nausea

MildUncommon

Limitations & Open Questions

Cardarine is not a peptide and is not FDA approved. Clinical data are limited to one short human trial; the program was discontinued after rodent carcinogenicity findings, and no long-term human outcome or safety data exist. Any dosing advice circulating online has no clinical support.

Pharmacology

Oral small-molecule PPARδ (PPARβ/δ) agonist; GW501516 activates PPARδ nuclear-receptor signaling to upregulate fatty-acid-oxidation genes. Human pharmacokinetic data are limited to short-term study protocols; it is not a peptide and has no approved dose.

Reported Research Dosing

Reported values from research literature and community protocols. Educational reference only — not a dosing recommendation or medical advice.

10-20mg daily

Route: Oral
Half-life: 24 hours

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

4
Differential effects of selective- and pan-PPAR agonists on experimental steatohepatitis and hepatic macrophages().

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)

+ 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.

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