Cardarine (GW-501516)

Overview

Cardarine (GW-501516) is a synthetic small-molecule PPARδ agonist — not a SARM and not a peptide, despite gray-market marketing that groups it with SARMs. GSK took it into human lipid trials but discontinued development around 2007 after rodent carcinogenicity findings. It has no regulatory approval, is WADA-prohibited at all times, and is sold only as a gray-market research chemical.

Mechanism of Action

GW-501516 is a potent, subtype-selective agonist of PPARδ (PPARβ/δ). In skeletal muscle it activates PGC-1-dependent programs for fatty-acid uptake, β-oxidation, and mitochondrial energy uncoupling; in macrophages it induces ABCA1 and reverse cholesterol transport. It does not act on the androgen receptor and is not a SARM. The carcinogenicity signal that ended its development is corroborated by a 2019 mouse colorectal-cancer study.

Research Summary

Completed GSK-sponsored human trials in low-HDL/dyslipidemia subjects (2.5–10 mg/day, 12 weeks) improved lipids (HDL-C +16.9%, triglycerides −16.9%, LDL −7.3%; Sprecher et al., 2012). GSK halted development around 2007 after a 2-year rodent carcinogenicity study reported tumors across multiple organs; a 2019 mouse study found GW-501516 accelerated colitis-associated colorectal cancer. A published human case report documented severe rhabdomyolysis and hepatotoxicity from self-administration. Never approved for any indication; not a peptide.

Vendors selling Cardarine (GW-501516)

Scored vendors carrying Cardarine (GW-501516), ranked by trust grade. Grades are computed from indexed Certificates of Analysis. Full $/mg pricing is on the comparison page.

Reported Side Effects

• Rodent carcinogenicity (tumors across multiple organs) ended clinical development — the central safety signal
• Documented human harm from self-administration: severe rhabdomyolysis and hepatotoxicity (case report)
• WADA-prohibited at all times (S4.4.1 metabolic modulators)
• No controlled human safety data outside the terminated GSK lipid trials

Compare Cardarine (GW-501516) with Others

Research References

• Narkar VA, et al. AMPK and PPARδ agonists are exercise mimetics. Cell. 2008. PMID 18674809.
• Sprecher DL, et al. Lipid effects of GW501516 in subjects with low HDL cholesterol. ATVB. 2012. PMID 22814748.
• Zhou X, et al. PPARδ agonist enhances colitis-associated colorectal cancer. Eur J Pharmacol. 2019. PMID 30391747.
• GW1516 (Cardarine) + MK-2866 human case report — severe rhabdomyolysis and hepatotoxicity. 2021. PMC8538264.

Frequently asked questions

Has Cardarine (GW-501516) been independently lab-tested?

Disclosed Labs has collected 2 Certificates of Analysis (COA) for Cardarine (GW-501516) from 1 independent testing lab. 1 vendor has submitted material for testing. Products average 99.7% tested purity across the corpus. Full testing data is available at https://www.disclosedlabs.com/peptides/gw-501516/testing.

Where can researchers source Cardarine (GW-501516)?

1 vendor with Disclosed Labs trust grades currently list Cardarine (GW-501516), including Kimera Chems. Compare live prices and lab-verified COAs at https://www.disclosedlabs.com/prices/gw-501516.

How does Cardarine (GW-501516) work?

GW-501516 is a potent, subtype-selective agonist of PPARδ (PPARβ/δ). In skeletal muscle it activates PGC-1-dependent programs for fatty-acid uptake, β-oxidation, and mitochondrial energy uncoupling; in macrophages it induces ABCA1 and reverse cholesterol transport. It does not act on the androgen receptor and is not a SARM. The carcinogenicity signal that ended its development is corroborated by a 2019 mouse colorectal-cancer study.

What does the research say about Cardarine (GW-501516)?

Completed GSK-sponsored human trials in low-HDL/dyslipidemia subjects (2.5–10 mg/day, 12 weeks) improved lipids (HDL-C +16.9%, triglycerides −16.9%, LDL −7.3%; Sprecher et al., 2012). GSK halted development around 2007 after a 2-year rodent carcinogenicity study reported tumors across multiple organs; a 2019 mouse study found GW-501516 accelerated colitis-associated colorectal cancer. A published human case report documented severe rhabdomyolysis and hepatotoxicity from self-administration. Never approved for any indication; not a peptide.