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PPARδ Agonist

Cardarine

Overview

An endurance/lipid compound whose clinical development was discontinued after long-term rodent studies showed cancers across multiple organs; banned in sport.

How it works

Cardarine (GW-501516) is not a SARM or a hormone — it's a PPARδ agonist. PPARδ is a 'nuclear receptor' that acts like a master switch for genes controlling how cells use fat for fuel.

By turning on PPARδ, it ramps up the genes for burning fatty acids and building mitochondria in muscle, which in animals dramatically increased endurance and improved cholesterol — the origin of its 'exercise in a bottle' reputation.

Here the most important fact isn't the benefit, it's the safety finding: long-term rodent studies showed it caused cancers in multiple organs, which led the developer to abandon it entirely around 2007. It's banned in sport, and that carcinogenicity signal is the dominant reason it should be regarded as dangerous rather than promising.

Mechanism · Detailed Analysis
Molecular targetA potent, selective agonist of the PPARδ (PPARβ/δ) nuclear receptor.
Signaling & downstream effectsHeterodimerises with RXR and drives transcription of fatty-acid-oxidation, mitochondrial, and energy-uncoupling genes in muscle — the basis for its endurance and lipid effects.
CaveatsLong-term rodent studies showed cancers across multiple organs at doses ≥3 mg/kg/day, mechanistically tied to PPARδ-driven proliferation. Development was abandoned and it is banned in sport. This carcinogenicity finding is the dominant fact.
Published EvidenceLoading cited studies from PubMed…
Human Data ···

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Animal ···

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In Vitro ···

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Educational aggregation of public literature. Not medical advice and not a recommendation to use any compound. Many compounds here are not approved for human use. Consult a licensed clinician.