GW‑501516 (Cardarine)
PPARδ-agonist GlaxoSmithKline candidate (NOT AR-binding). GSK 2007 internal Sprague-Dawley rat 2-year carcinogenicity (intestinal + hepatocellular tumors, dose-dependent) → Phase II terminated (Sprenger 2010 PMID 20189836). RESEARCH-ONLY chemical, do not use; WADA S4.5 banned since 2009.
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WHAT IS GW-501516 (CARDARINE)?
Detailed overview
GW-501516 (Cardarine, GW1516) is a PPARδ-selective agonist developed by GlaxoSmithKline (GSK) in the late 1990s within their dyslipidemia + metabolic-syndrome Rx-indication pipeline. PPARδ (peroxisome proliferator-activated receptor delta) is a nuclear receptor expressed in skeletal muscle + hepatocytes + endothelial cells; its activation upregulates fatty-acid oxidation + glucose utilization, generating the preclinical 'exercise-mimetic' hype (Geiger 2008 Cell PMID 18674809, Narkar 2008 Cell PMID 18674806 – replicated evidence base in mouse models). NOT AR-binding (NOT SARM, NOT a steroid). The clinical program was terminated in 2007: GSK's internal 2-year Sprague-Dawley rat carcinogenicity study showed dose-dependent intestinal + hepatocellular tumor formation at every tested dose level (Sprenger 2010 J Lipid Res PMID 20189836 published the Phase II termination context). Human-trial 2-year carcinogenicity data is NOT available – research-ethics committees block long-term human Phase III based on the rat data. WADA S4.5 banned since 2009 (USADA banlist update). FDA Consumer Warning 2013 also warns under the SARMs-related category, because the research-chemical underground market continues to sell it online as 'cardarine 10-20 mg/cap' with label-claim discrepancy. RESEARCH-ONLY chemical – do not use; since the Phase II termination + WADA ban, the risk-benefit ratio is clinically negative.
Mechanism
PPARδ-selective agonist (NOT AR-binding, NOT SARM, NOT a steroid)
Dosing
Research-context only 10-20 mg/day PO (FDA never approved, NO human Rx dose)
Half-life
~24h (from preclinical data, limited human PK)
Onset
Preclinical: lipid-profile shift 2-4 weeks (extrapolated from mouse model)
Legal status
FDA never approved (Phase II terminated 2007); EU EMA never approved; research-chemical underground market only. WADA S4.5 banned since 2009.
Data console
Lab data
Safety
Side effects, stop signs, contraindications
Side effects · 6
- Carcinogenic potential (most serious): GSK 2-year Sprague-Dawley rat bioassay showed dose-dependent, multi-tissue tumor formation (intestine, liver, bladder, skin, tongue) at every dose tested. No human data, but this caused Phase II termination.
- Absent human safety data: the clinical program stopped in 2007, no long-term human toxicity or tumor-latency data exists. The risk-benefit ratio is clinically negative; this is a research-only chemical.
- Possible hepatic burden: due to preclinical hepatocellular tumor formation and hepatic PPARδ activation, liver enzyme (ALT/AST/GGT) elevation is plausible, though not documented in human trials.
- Increased sweating: the most commonly reported (anecdotal) non-serious complaint in user reports; community experience, not clinical evidence.
- Quality and purity risk: no pharmacy source, only a research-chemical gray market. Declared content often does not match reality (in SARM-related analogs an RCT found ~27% of products did not contain the labeled compound); contaminated batches are a real hazard.
- Sport sanction (WADA): banned since 2009 (S4.5 hormone and metabolic modulators). Accredited LC-MS/MS urine testing detects it for 2-4 weeks; a positive result means a competition ban.
Contraindications · 6
- Human consumption in general: due to the 2-year multi-tissue rat carcinogenicity and the terminated clinical program there is no safe human protocol; research-only chemical. Do not use.
- Any malignancy history or active cancer: absolute contraindication due to the dose-dependent preclinical tumor formation.
- Pre-existing liver disease: absolute contraindication due to preclinical hepatocellular tumor formation and hepatic PPARδ activation.
- Pregnancy and breastfeeding: no human reproductive safety data; contraindicated due to the carcinogenic signal and risk to the developing organism.
- Competitive athletes (in- and out-of-competition): WADA S4.5 banned substance since 2009, detectable by accredited urine testing.
- Concurrent alcohol or other hepatotoxic agents (e.g. oral 17-alpha-alkylated steroids): hepatic stress is additive, to be avoided.
Related Performance Compounds
Same therapeutic category
Studies
Related research and clinical findings
AMPK and PPARdelta agonists are exercise mimetics.
Narkar VA, Downes M, Yu RT, Embler E, Wang YX, Banayo E, Mihaylova MM, Nelson MC, Zou Y, Juguilon H, Kang H, Shaw RJ, Evans RM
Regulation of muscle fiber type and running endurance by PPARdelta.
Wang YX, Zhang CL, Yu RT, Cho HK, Nelson MC, Bayuga-Ocampo CR, Ham J, Kang H, Evans RM
Induction of metastatic gastric cancer by peroxisome proliferator-activated receptorδ activation.
Pollock CB, Rodriguez O, Martin PL, Albanese C, Li X, Kopelovich L, Glazer RI
Dual acting and pan-PPAR activators as potential anti-diabetic therapies.
Heald M, Cawthorne MA
WADA prohibited list update – S4.5 hormone and metabolic modulators (GW501516 ban 2009)
WADA / USADA banlist update.
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The information here is for educational and scientific purposes only. Performance-enhancing compounds (AAS, prohormones, stimulants, doping agents) are illegal without prescription in Hungary and most of the EU, and carry serious health and legal risks. WADA bans them in competitive sport. This is NOT a usage guide, and we do not encourage any illegal use. If you do use them, medical supervision and regular bloodwork are ESSENTIAL. Severe endocrine, cardiovascular, hepatic and psychiatric side effects are possible.